Use of an inhibitor of the Na+/H+ exchanger for the production of a medicament for the treatment or prophylaxis of disturbances of the central nervous system

ABSTRACT

The use of an inhibitor of the Na + /H +  exchanger for the production of a medicament for the treatment or prophylaxis of disorders of the central nervous system. Inhibitors of the Na + /H +  exchanger are outstandingly suitable for the production of a medicament for the treatment or prophylaxis of disorders of the central nervous system; derivatives of guanidine are particularly highly suitable; cariporide (HOE 642) is especially suitable.

[0001] The use of an inhibitor of the Na⁺/H⁺ exchanger for theproduction of a medicament for the treatment or prophylaxis ofdisturbances of the central nervous system

[0002] The invention describes the use of inhibitors of the cellularsodium-hydrogen exchanger for the production of a medicament for thetherapy and prophylaxis of disorders and disturbances which are causedby hyperexcitability of the central nervous system, in particular forthe treatment of disorders of the epileptic type, centrally inducedclonic and tonic spasms, anxiety disorders and psychoses.

[0003] Inhibitors of the sodium/hydrogen exchanger (NHE) have recentlybeen characterized in numerous preclinical studies as substances whichin the case of restricted circulation of the heart are suitable in asuperior manner to protect endangered heart tissue from death. Theprotection of the heart tissue by NHE inhibitors includes allexpressions of the damage caused by the inadequate circulation, startingwith cardiac arrhythmias via hypercontraction of the heart muscle andtemporary loss of function up to death of the heart tissue and permanentdamage associated therewith.

[0004] The mechanism of action of the NHE inhibitors is that theydecrease the increased sodium ion influx which arises in inadequatelysupplied tissues due to activation of the NHE as a result ofintracellular acidification. The situation of sodium overloading of thetissue is thereby delayed. Since sodium and calcium ion transport arecoupled to one another in the heart tissue, the life-threatening calciumoverloading of the heart cells is thus prevented.

[0005] In the same manner as in the heart, a protection of the centralnervous system under the influence of inhibitors of the NHE has likewisealready been described in most of the patents cited here, activecompounds of this type protecting the CNS similarly to the heart againstischemic conditions. These conditions are caused by an inadequatecirculation and thus by an inadequate supply of nutrients, oxygen,minerals etc. Ischemic damage to the CNS of this type is particularlymarked in the case of central nervous system infarcts, such as stroke.

[0006] In the case of normal healthy circulation, as expected, it wastherefore, of course, also not possible to observe any protectiveeffects of NHE inhibitors, since no ischemic tissue damage to the heartor to the CNS occurred.

[0007] It was therefore surprising that NHE inhibitors, beside theprotective effects which only have an influence under conditions ofinadequate circulation, also still have direct therapeuticallyutilizable actions against disorders and disturbances of the CNS whichare independent of inadequate circulation states and occur in normal,nonischemic conditions. These pathological, nonischemically inducedsymptoms, which recently have been made accessible to treatment with NHEinhibitors, are disorders and disturbances which are substantiallycaused by a hyperexcitability of neurons of the central nervous system.NHE inhibitors act on disorders and disturbances of this type by adamping of the hyperactivity of CNS neurons.

[0008] Disturbances in which an inhibition of the excitability of thehyperactive neurons plays a dominant part include those of the epileptictype, for example grand mal, petit mal etc.

[0009] Neuronal hyperactivity, however, is not only observed inepilepsy. In other centrally induced functional disturbances such as invarious psychoses, neuronal hyperactivity in various brain regions isalso suspected as a cause. Since the described principle of action ofthe inhibition of the NHE can damp the neuronal hyperactivityindependently of the trigger or disease, it is suitable not only for thetherapy of epilepsies, but also for the treatment of affective psychosesand anxiety disturbances. The indications resulting therefrom thusinclude the treatment of epilepsies and affective psychoses and anxietydisturbances.

[0010] The NHE inhibitors employed antiepileptically andantipsychotically can be used on their own. The unique mechanism ofaction of the NHE inhibitors also makes it possible, however, to combineNHE inhibitors with other active compounds which are based on anothermechanism of action. Thus, for example, combinations of NHE inhibitorswith other substances having antiepileptic action or antipsychoticactive compounds, or carboanhydrase inhibitors (e.g. acetazolamide)allow favorable therapy schemes and treatment results which are notattainable using the individual components of the combination.

[0011] In the model of CA3 neurons in hippocampus tissue slices, NHEinhibitors with their antiepileptic and antipsychotic therapy potentialinhibit epileptiform discharges. Hyperexcitability of neurons in theform of so-called epileptiform discharges was triggered by the action ofbicuculline, caffeine or low magnesium concentrations. HOE 642, ablocker of the Na⁺/H⁺ isoform1, showed a marked inhibition of theepileptiform discharges caused by the excitatory action of thesesubstances.

[0012] Experimental demonstration of action of the damping of neuronalexcitation states by NHE inhibitors:

[0013] The decrease in neuronal excitability was tested on slicepreparations of CA3 neurons of the hippocampus (guinea-pigs). Theexcitation-inhibiting action of cariporide (HOE 642) was investigated in8 experiments. The neuronal excitability was assessed with intracellularleads with the aid of the spontaneous bioelectric activity and thepharmacologically produced epileptiform activity which had been inducedby bicuculline, caffeine or absence of magnesium. Both the frequency ofthe spontaneous action potentials and the frequency of so-calledperiodic paroxysmal depolarization was clearly reversibly reduced by30-80% for more than 45 minutes after a wash-in time of 0.1-0.5 mMcariporide.

[0014] A relationship between neuronal excitability and inhibition ofthe Na⁺/H⁺ exchanger is already indicated in “Suppressive Action ofpropionate and inhibitors of cellular acid-extrusion mechanisms (IAE) onepileptiform activity of CA3 neurons, Eur. J. Physiol. R 153, P-562,1997; however, the action of the guanidines and similar compounds isneither anticipated nor suggested by this.

[0015] The active compounds known and identified as NHE inhibitors areguanidine derivatives, preferably acylguanidines, inter alia asdescribed in the following publications and patent disclosures: EdwardJ. Cragoe, Jr., “DIURETICS, Chemistry, Pharmacology and Medicine”, J.WILEY & Sons (1983), 303-341, additionally compounds of the followingformulae:

[0016] I. (HOE 89/F 288—U.S. Pat. No. 5,292,755)

[0017] a) benzoylguanidines of the formula I

[0018] in which:

[0019] R(1) or R(2)

[0020] is R(6)—S(O)_(n)— or R(7)R(8)N—O₂S—;

[0021] and the other substituent R(1) or R(2) in each case

[0022] is H, F, Cl, Br, (C₁-C₄)-alkyl, (C₁-C₄)-alkoxy or phenoxy,

[0023] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of fluorine, chlorine, methyl andmethoxy;

[0024] or the other substituent R(1) or R(2) in each case

[0025] is R(6)—S(O)_(n) or R(7)R(8)N—;

[0026] n is zero, 1 or 2;

[0027] R(6) is (C₁-C₆)-alkyl, (C₅-C₇)-cycloalkyl, cyclopentylmethyl,cyclohexylmethyl or phenyl,

[0028] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of fluorine, chlorine, methyl andmethoxy;

[0029] R(7) and R(8)

[0030] identically or differently are H or (C₁-C₆)-alkyl;

[0031] or

[0032] R(7) is phenyl-(CH₂)_(m);

[0033] m is 1-4;

[0034] or

[0035] R(7) is phenyl,

[0036] which is unsubstituted or substituted by 1-2 substituentsselected from the group consisting of fluorine, chlorine, methyl andmethoxy;

[0037] or

[0038] R(7) and R(8)

[0039] together are a straight-chain or branched (C₄-C₇)-chain, wherethe chain can additionally be interrupted by O, S or NR(9);

[0040] R(9) is H or methyl;

[0041] or

[0042] R(7) and R(8)

[0043] together with the nitrogen atom to which they are bonded, are adihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system;

[0044] R(3), R(4) and R(5)

[0045] independently of one another are H or (C₁-C₂)-alkyl,

[0046] or

[0047] R(3) and R(4)

[0048] together are a (C₂-C₄)-alkylene chain;

[0049] or

[0050] R(4) and R(5)

[0051] together are a (C₄-C₇)-alkylene chain;

[0052] and their pharmaceutically tolerable salts;

[0053] (HOE 92/F 34—U.S. Pat No. 5,373,924)

[0054] b) benzoylguanidines of the formula I

[0055] in which:

[0056] R(1) is R(4)—SO_(m) or R(5)R(6)N—SO₂—;

[0057] m is zero, 1 or 2;

[0058] R(4) and R(5)

[0059] are C₁-C₈-alkyl, C₃-C₆-alkenyl or —C_(n)H_(2n)—R(7);

[0060] n is zero, 1, 2, 3 or 4;

[0061] R(7) is C₅-C₇-cycloalkyl or phenyl,

[0062] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[0063] R(8) and R(9)

[0064]  are H or C₁-C₄-alkyl;

[0065] or

[0066] R(5) is H;

[0067] R(6) is H or C₁-C4-alkyl,

[0068] or

[0069] R(5) and R(6)

[0070] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by an O, S, NH, N—CH₃ or N-benzyl;

[0071] R(2) is hydrogen, F, Cl, Br, (C₁-C₄)-alkyl-,O—(CH₂)_(m)C_(p)F_(2p+1) or —X—R(10);

[0072] m is zero or 1;

[0073] p is 1, 2 or 3;

[0074] X is O, S or NR(11);

[0075] R(10) is H, C₁-C₆-alkyl, C₅-C₇-cycloalkyl, cyclohexylmethyl,cyclopentylmethyl or —C_(n)H_(2n)—R(12);

[0076] n is zero, 1, 2, 3 or 4;

[0077] R(12) is phenyl,

[0078] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9); R(8) and R(9)

[0079]  are H or C₁-C₄-alkyl;

[0080] R(11) is hydrogen or C₁-C₃-alkyl;

[0081] or

[0082] R(10) and R(11)

[0083] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by O, S, NH, N—CH₃ or N-benzyl;

[0084] R(3) is defined as R(1), or is C₁-C₆-alkyl, nitro, cyano,trifluoromethyl, F,

[0085] Cl, Br, I or —X—R(10);

[0086] X is O, S or NR(11);

[0087] R(10) is H, C₁-C₆-alkyl, C₅-C7-cycloalkyl, cyclohexylmethyl,cyclopentylmethyl or —C_(n)H_(2n)—R(12);

[0088] n is zero to 4;

[0089] R(12) is phenyl,

[0090] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[0091] R(8) and R(9)

[0092]  are H or C₁-C₄-alkyl;

[0093] R(11) is C₁-C₃-alkyl,

[0094] or

[0095] R(10) and R(11)

[0096] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by O, S, NH, N—CH₃ or N-benzyl;

[0097] and their pharmaceutically tolerable salts;

[0098] (HOE 92/F 035 EP-A 556 673)

[0099] c) ortho-substituted benzoylguanidines of the formula I

[0100] in which:

[0101] R(1) is F, Cl, Br, I, C₁-C₆-alkyl or —X—R(6);

[0102] X is O, S, NR(7) or Y—ZO;

[0103] Y is O or NR(7);

[0104] Z is C or SO;

[0105] R(6) is H, C₁-C₆-alkyl, C₅-C₇-cycloalkyl, cyclohexylmethyl,cyclopentylmethyl, —(CH₂)_(m)C_(p)F_(2p+1) or —C_(n)H_(2n)—R(8);

[0106] m is zero or 1;

[0107] p is 1-3;

[0108] n is zero to 4;

[0109] R(8) is phenyl,

[0110] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of the groups F, Cl, CF₃, methyl,methoxy and NR(9)R(10);

[0111] R(9) and R(10)

[0112]  are H or C₁-C₄-alkyl;

[0113] R(7) is H or C₁-C₃-alkyl;

[0114] or

[0115] R(6) and R(7)

[0116] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by O, S, NH, N—CH₃ or N-benzyl;

[0117] R(3) is H or —X—R(6);

[0118] X is O, S, NR(7) or Y—ZO;

[0119] R(7) is H or C₁-C₃-alkyl;

[0120] Y is O or NR(7);

[0121] where Y is bonded to the phenyl radical of the formula I,

[0122] Z is C or SO;

[0123] R(6) is H, C₁-C₆-alkyl, C₅-C₇-cycloalkyl, cyclohexylmethyl,cyclopentylmethyl, —(CH₂)_(m)C_(p)F_(2p+1) or —C_(n)H_(2n)—R(8);

[0124] m is zero or 1;

[0125] p is 1-3;

[0126] n is zero to 4;

[0127] R(8) is phenyl,

[0128] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10);

[0129] R(9) and R(10)

[0130]  are H or C₁-C₄-alkyl;

[0131] or

[0132] R(6) and R(7)

[0133] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by O, S, NH, N—CH₃ or N-benzyl;

[0134] R(2) and R(4)

[0135] identically or differently are R(11)—SO_(q)— or R(12)R(13)N—SO₂—;

[0136] q is zero-2;

[0137] R(11) is C₁-C₄-alkyl,

[0138] which is unsubstituted or carries phenyl as a substituent, wherephenyl is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(9)R(10);

[0139] R(9) and R(10)

[0140]  are H or C₁-C₄-alkyl;

[0141] R(12) and R(13)

[0142] are defined as R(6) and R(7);

[0143] or one of the two radicals R(2) or R(4)

[0144] is hydrogen or is defined as R(1);

[0145] R(5) is H, methyl, F, Cl or methoxy,

[0146] and their pharmaceutically tolerable salts;

[0147] (HOE 92/F 036—U.S. Pat. No. 5,364,868)

[0148] d) benzoylguanidines of the formula I

[0149] in which:

[0150] R(1) or R(2)

[0151] is an amino group —NR(3)R(4);

[0152] R(3) and R(4)

[0153] identically or differently are H, C₁-C₆-alkyl orC₃-C₇-cycloalkyl;

[0154] or

[0155] R(3) is phenyl-(CH₂)_(p)—;

[0156] p is 0, 1 , 2, 3 or 4;

[0157] or

[0158] R(3) is phenyl,

[0159] where the phenyl in each case is unsubstituted or carries one totwo substituents selected from the group consisting of fluorine,chlorine, methyl and methoxy;

[0160] or

[0161] R(3) and R(4)

[0162] together can be a straight-chain or branched C₄-C₇-methylenechain, where one —CH₂— member of the methylene chain can be replaced byoxygen, S or NR(5);

[0163] R(5) is H or lower alkyl;

[0164] the other substituent R(1) or R(2) in each case

[0165] is H, F, Cl, C₁-C₄-alkyl, C₁-C₄-alkoxy, CF₃, C_(m)F_(2m+1)—CH₂—,benzyl or phenoxy,

[0166] where the respective phenyl radical is unsubstituted or carriesone to two substituents selected from the group consisting of methyl,methoxy, fluorine and chlorine;

[0167] m is 1, 2 or 3;

[0168] and their pharmaceutically tolerable salts;

[0169] (92/F 197 K—NZ 248 013)

[0170] e) benzoylguanidines of the formula I

[0171] in which:

[0172] R(1) is R(4)—SO_(m) or R(5)R(6)N—SO₂—;

[0173] m is zero, 1 or 2;

[0174] R(4) and R(5)

[0175] are C₁-C₈-alkyl, C₃-C₆-alkenyl or —C_(n)H_(2n)—R(7);

[0176] n is zero, 1, 2, 3 or 4;

[0177] R(7) is C₅-C₇-cycloalkyl or phenyl,

[0178] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[0179] R(8) and R(9)

[0180]  are H or C₁-C₄-alkyl;

[0181] or

[0182] R(5) is H;

[0183] R(6) is H or C₁-C₄-alkyl;

[0184] or

[0185] R(5) and R(6)

[0186] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by an O, S, NH, N—CH₃ or N-benzyl;

[0187] R(2) is hydrogen, straight-chain or branched (C₅-C₈)-alkyl,—CR(13)═CHR(12) or —C≡CR(12);

[0188] R(12) is phenyl,

[0189] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(14)R(15);

[0190] R(14) and R(15)

[0191] are H or (C₁-C₄)-alkyl;

[0192] or

[0193] R(12) is (C₁-C₉)-heteroaryl,

[0194] which is unsubstituted or substituted as phenyl,

[0195] or

[0196] R(12) is (C₁-C₆)-alkyl,

[0197] which is unsubstituted or substituted by 1-3 OH,

[0198] or

[0199] R(12) is (C₃-C₈)-cycloalkyl;

[0200] R(13) is hydrogen or methyl,

[0201] or

[0202] R(12) is (C₃-C₈)-cycloalkyl, (C₃-C₈)-cycloalkyl-(C₁-C₄)-alkyl,phenyl,

[0203] C₆H₅—(C₁-C₄)-alkyl, naphthyl, biphenylyl,1,1-diphenyl-(C₁-C₄)-alkyl, cyclopentadienyl, pyridyl, pyrrolyl,furanyl, thienyl, thiazolyl, oxazolyl, indenyl, quinolyl, indolyl,benzofuranyl, benzothienyl, benzothiazolyl, benzoxazolyl, imidazolyl,pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, pyrazinyl,pyrimidinyl, pyridazinyl, indazolyl, isoquinolyl, phthalazinyl,quinoxalinyl, quinazolinyl or cinnolinyl;

[0204] R(3) is defined as R(2);

[0205] and where the aromatic substituents R(2) and R(3) areunsubstituted or substituted by 1-3 substituents from the groups F, Cl,CF₃, (C₁-C₄)-alkyl or -alkoxy, or NR(10)R(11) with R(10) and R(11) beingH or (C₁-C₄)-alkyl;

[0206] and their pharmaceutically tolerable salts;

[0207] (HOE 92/F 303 K—EP-A 589 336, NZ 248 703)

[0208] f) benzoylguanidines of the formula I

[0209] in which:

[0210] R(1) or R(2)

[0211] is R(3)—S(O)_(n)— or R(4)R(5)N—SO₂—

[0212] the other substituent R(1) or R(2) in each case

[0213] is H, OH, F, Cl, Br, I, C₁-C₄-alkyl, C₁-C₄-alkoxy, benzyloxy orphenoxy,

[0214] which is unsubstituted or carries one to three substituentsselected from the group consisting of fluorine, chlorine, methyl,methoxy, hydroxyl or benzyloxy,

[0215] R(3)—S(O)_(n), —NR(4)R(5) or 3,4-dehydropiperidine

[0216] R(3) is C₁-C₆-alkyl, C5-C₇-cycloalkyl, cyclopentylmethyl,

[0217] cyclohexylmethyl or phenyl,

[0218] which is unsubstituted or carries one to three substituentsselected from the group consisting of fluorine, chlorine, methyl andmethoxy;

[0219] R(4) and R(5)

[0220] identically or differently, are H or C₁-C₆-alkyl;

[0221] or

[0222] R(4) is phenyl-(CH₂)_(m)—;

[0223] m is 1, 2, 3 or 4;

[0224] or

[0225] R(4) is phenyl,

[0226] which is unsubstituted or carries one to two substituentsselected from the group consisting of fluorine, chlorine, methyl andmethoxy;

[0227] or

[0228] R(4) and R(5)

[0229] together are a straight-chain or branched C₄-C₇-chain, where thechain can additionally be interrupted by O, S or NR(6),

[0230] R(6) is H or methyl;

[0231] or

[0232] R(4) and R(5)

[0233] together with the nitrogen atom to which they are bonded, are adihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system;

[0234] n is zero, 1 or 2;

[0235] and their pharmaceutically tolerable salts;

[0236] (92/F 304—U.S. Pat. No. 5,416,094)

[0237] g) isoquinolines of the formula I

[0238] in which:

[0239] R(1) is hydrogen, alkyl, cycloalkyl, arylalkyl, alkenyl,substituted aminoalkyl or an aryl or heteroaryl ring;

[0240] where the rings are unsubstituted or substituted by 1-3 groupsselected from the group consisting of halogen, nitro, amino, mono(loweralkyl)amino, di(lower alkyl)amino, lower alkyl, lower alkoxy, benzyloxy,phenoxy, hydroxyl, trifluoromethyl,

[0241] R(2) is hydrogen, halogen, alkyl or aryl;

[0242] which is unsubstituted or substituted by 1-3 groups selected fromthe group consisting of halogen, nitro, amino, mono(lower alkyl)amino,di(lower alkyl)amino, lower alkyl, lower alkoxy, benzyloxy, phenoxy,hydroxyl,

[0243] G is —N═C{[NR(3)R(4)][N(R5)R(6)]};

[0244] R(3), R(4), R(5) and R(6) are hydrogen,

[0245] X(2), X(3) and X(4)

[0246] independently of one another are hydrogen, halogen, nitro, amino,alkyl, sulfonamide, mono(lower alkyl)amino, di(lower alkyl)amino, loweralkyl, benzyloxy, hydroxyl;

[0247] X(1) is hydrogen, oxygen, sulfur or NR(7);

[0248] R(7) is hydrogen, alkyl, cycloalkyl, arylalkyl, alkenyl,substituted aminoalkyl or an aryl or a heteroaryl ring;

[0249] which rings are unsubstituted or substituted by 1-3 groupsselected from the group consisting of halogen, nitro, amino, mono(loweralkyl)amino, di(lower alkyl)amino, lower alkyl, lower alkoxy, benzyloxy,phenoxy, hydroxyl and trifluoromethyl;

[0250] in which substituents each alkyl chain or alkenyl chain can beinterrupted by oxygen, sulfur or NR(8);

[0251] R(8) is hydrogen, alkyl, cycloalkyl, arylalkyl, alkenyl,substituted aminoalkyl or an aryl or heteroaryl ring,

[0252] which rings are unsubstituted or substituted by 1-3 groupsselected from the group consisting of halogen, nitro, amino, mono(loweralkyl)amino, di(lower alkyl)amino, lower alkyl, lower alkoxy, benzyloxy,phenoxy, hydroxyl and trifluoromethyl;

[0253] and their pharmaceutically acceptable salts;

[0254] (92/F 404—EP 602 522, NZ 250 438)

[0255] h) compounds of the formula I

[0256] in which:

[0257] R(1) is hydrogen, F, Cl, Br, I, —NO₂, —C≡N, —CF₃, R(4)—SO_(m) or

[0258] R(5)R(6)N—SO₂—;

[0259] m is zero, 1 or 2;

[0260] R(4) and R(5)

[0261] are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(7) or CF₃;

[0262] n is zero, 1, 2, 3 or 4;

[0263] R(7) is (C₃-C₇)-cycloalkyl or phenyl,

[0264] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[0265] R(8) and R(9)

[0266]  are H or C₁-C₄-alkyl;

[0267] or

[0268] R(5) is H;

[0269] R(6) is H or (C₁-C₄)-alkyl;

[0270] or

[0271] R(5) and R(6)

[0272] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0273] R(2) is —SR(10), —OR(10), —NHR(10), —NR(10)R(11), —CHR(10)R(12),—[CR(12)R(13)OR(13′)], —{C—[CH₂—OR(13′)]R(12)(R(13)} or—[CR(18)R(17)]_(p)—(CO)—[CR(19)R(20)]_(q)—R(14);

[0274] R(10) and R(11)

[0275] identically or differently are—[CHR(16)]_(s)—(CH₂)_(p)—(CHOH)_(q)—(CH₂)_(r)—(CHOH)_(t)—R(21) or—(CH₂)_(p)—O—(CH₂—CH₂O)_(q)—R(21),

[0276] R(21) is hydrogen, methyl,

[0277] p, q, r identically or differently

[0278] are zero, 1, 2, 3 or 4;

[0279] s is zero or 1;

[0280] t is 1, 2, 3 or 4;

[0281] R(12) and R(13)

[0282] identically or differently are hydrogen, (C₁-C₆)-alkyl or,together with the carbon atom carrying them, are a (C₃-C₈)-cycloalkyl,

[0283] R(13′) is hydrogen or (C₁-C₄)-alkyl;

[0284] R(14) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(a)H_(2a)—R(15);

[0285] a is zero, 1, 2, 3 or 4;

[0286] R(15) is phenyl,

[0287] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[0288] R(8) and R(9)

[0289]  are H or (C₁-C₄)-alkyl;

[0290] or

[0291] R(15) is (C₁-C₉)-heteroaryl,

[0292] which is unsubstituted or substituted as phenyl,

[0293] or

[0294] R(15) is (C₁-C₆)-alkyl,

[0295] which is unsubstituted or substituted by 1-3 OH;

[0296] R(16), R(17), R(18), R(19) and R(20)

[0297] are hydrogen or (C₁-C₃)-alkyl;

[0298] R(3) is defined as R(1),

[0299] or

[0300] R(3) is (C₁-C₆)-alkyl or —X—R(22);

[0301] X is oxygen, S or NR(16);

[0302] R(16) is H or (C₁-C₃)-alkyl;

[0303] or

[0304] R(22) and R(16)

[0305] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0306] R(22) is defined as R(14);

[0307] and their pharmaceutically tolerable salts;

[0308] (HOE 92/F 405—EP 602 523, NZ 250 437)

[0309] i) benzoylguanidines of the formula I

[0310] in which:

[0311] R(1) is hydrogen, F, Cl, Br, I, —NO₂, —C≡N,R(16—C_(p)H_(2p)—O_(q), R(4)—SO_(m) or R(5)R(6)N—SO₂—;

[0312] m is zero, 1 or 2;

[0313] p is zero or 1;

[0314] q is zero, 1, 2 or 3;

[0315] R(16) is C_(r)F_(2r+1);

[0316] r is 1, 2 or 3;

[0317] R(4) and R(5)

[0318] are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(7) or CF₃;

[0319] n is zero, 1, 2, 3 or 4;

[0320] R(7) is (C₃-C₇)-cycloalkyl or phenyl,

[0321] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[0322] R(8) and R(9)

[0323]  are H or C₁-C₄-alkyl;

[0324] or

[0325] R(5) is H;

[0326] R(6) is H or (C₁-C₄)-alkyl;

[0327] or

[0328] R(5) and R(6)

[0329] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl,

[0330] R(2) is (C₁-C₉)-heteroaryl,

[0331] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[0332] or

[0333] R(2) is —SR(10), —OR(10), —NR(10)R(11), —CR(10)R(11)R(12);

[0334] R(10) is —C_(a)H_(2a)—(C₁-C₉)-heteroaryl,

[0335] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[0336] a is zero, 1 or 2;

[0337] R(11) and R(12)

[0338] independently of one another are defined as R(10) or are hydrogenor (C₁-C₄)-alkyl;

[0339] R(3) is defined as R(1), or is (C₁-C₆)-alkyl or —X—R(13);

[0340] X is oxygen, S, or NR(14);

[0341] R(14) is H or (C₁-C₃)-alkyl;

[0342] R(13) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(b)H_(2b)—R(15);

[0343] b is zero, 1, 2, 3 or 4;

[0344] or

[0345] R(13) and R(14)

[0346] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0347] R(15) is phenyl,

[0348] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[0349] R(8) and R(9)

[0350]  are H or (C₁-C₄)-alkyl;

[0351] and their pharmaceutically tolerable salts;

[0352] (HOE 92/F 411—NZ 250 450, EP 603 650)

[0353] k) benzoylguanidines of the formula I

[0354] in which:

[0355] one of the substituents R(1), R(2), R(3) or R(4):

[0356] is an amino group —NR(5)[C_(n)H_(2n)—R(6)];

[0357] R(5) is hydrogen or C₍₁₋₆₎-alkyl;

[0358] n is zero, 1, 2, 3 or 4;

[0359] R(6) is H or C₍₁₋₄₎-alkyl;

[0360] in which one CH₂ group can be replaced by 1 sulfur atom or agroup NR(7);

[0361] R(7) is hydrogen, methyl or ethyl;

[0362] or

[0363] R(6) is C₍₃₋₈₎-cycloalkyl or phenyl,

[0364] which is unsubstituted or carries 1, 2 or 3 substituents selectedfrom the group consisting of F, Cl, Br, methyl, methoxy, —NR(8)R(9);

[0365] R(8) and R(9)

[0366] are H, methyl or ethyl;

[0367] or

[0368] R(5) and R(6)

[0369] together with the nitrogen atom are a 5-, 6- or 7-membered ring,in which 1 carbon atom can be replaced by oxygen, S or NR(10);

[0370] R(10) is H, C₍₁₋₃₎-alkyl or benzyl;

[0371] and the other substituents R(1), R(2), R(3), R(4) in each caseare:

[0372] hydrogen, F, Cl, Br, I, CN, CF₃, NO₂, CF₃—O—,C_(m)F_(2m+1)—CH₂—O— or

[0373] R(11)—C_(q)H_(2q)—X_(p)—;

[0374] m is 1, 2 or 3;

[0375] q is zero, 1, 2, 3 or 4;

[0376] p is zero or 1;

[0377] X is oxygen or NR(12);

[0378] R(12) is H or C₍₁₋₃₎-alkyl;

[0379] R(11) is hydrogen, C₍₁₋₆₎-alkyl, C₍₃₋₈₎-cycloalkyl or phenyl,

[0380] which is unsubstituted or substituted by 1, 2 or 3 substituentsselected from the group consisting of F, Cl, CH₃, CH₃—O—and NR(13)R(14);

[0381] R(13) and R(14)

[0382] are H, methyl or ethyl;

[0383] and their pharmaceutically tolerable salts;

[0384] (HOE 921F 422—EP 604 852)

[0385] l) benzoylguanidines of the formula I

[0386] in which

[0387] R(1) is R(4)R(5)N—C(X)—;

[0388] X is oxygen, S or N—R(6);

[0389] R(4) and R(5)

[0390] identically or differently, are H, (C₁-C₈)-alkyl, (C₃-C₆)-alkenylor —C_(n)H₂—R(7);

[0391] n is zero, 1, 2, 3 or 4;

[0392] R(7) is (C₅-C₇)-cycloalkyl or phenyl,

[0393] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methoxy and(C₁-C₄)-alkyl;

[0394] or

[0395] R(4) and R(5)

[0396] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0397] R(6) is defined as R(4) or is amidine;

[0398] R(2) is H, F, Cl, Br, I, (C₁-C₈)-alkyl, 1-alkenyl or 1-alkynyl,(C₃-C₈)-cycloalkyl, (C₃-C₈)-cycloalkyl-(C₁-C₄)-alkyl, phenyl,C₆H₅—(C₁-C₄)-alkyl, naphthyl, biphenylyl, 1,1-diphenyl-(C₁-C₄)-alkyl,cyclopentadienyl, pyridyl, thiopyridyl, pyrrolyl, furanyl, thienyl,thiazolyl, oxazolyl, indenyl, quinolyl, indolyl, benzofuranyl,benzothienyl, benzothiazolyl, benzoxazolyl or —W—R(8);

[0399] W is oxygen, S or NR(9);

[0400] R(8) is H, (C₁-C₆)-alkyl, (C₅-C₇)-cycloalkyl, cyclohexylmethyl,cyclopentylmethyl, —(CH₂)_(m)C_(p)F_(2p+1) or —C_(q)H_(2q)—R(10);

[0401] m is zero or 1;

[0402] p is 1, 2 or 3;

[0403] q is zero, 1, 2, 3 or 4;

[0404] R(10) is phenyl,

[0405] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(11)R(12);

[0406] R(11) and R(12)

[0407]  are H or (C₁-C₄)-alkyl;

[0408] R(9) is H or (C₁-C₃)-alkyl;

[0409] or

[0410] R(8) and R(9)

[0411] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0412] R(3) is H, F, Cl, Br, I, (C₁-C₆)-alkyl or —W—R(8) as defined forR(2),

[0413] and their pharmaceutically acceptable salts;

[0414] (93/F 054—NZ 250 919, EP-A 612 723)

[0415] m) benzoylguanidines of the formula I

[0416] in which:

[0417] R(1), R(2), R(3)

[0418] are hydrogen, F, Cl, Br, I or (C₁-C₁₂)-alkyl;

[0419] one of the substituents R(1), R(2) or R(3)

[0420] is N₃, CN, OH or (C₁-C₁₀)-alkyloxy, if at least one of theremaining substituents R(1), R(2) or R(3) is a sufficiently lipophilicalkyl radical having 3 to 12 carbon atoms;

[0421] or

[0422] one of the substituents R(1), R(2) or R(3)

[0423] is R(4)—C_(n)H_(2n)—O_(m)—;

[0424] m is zero or 1;

[0425] n is zero, 1, 2 or 3;

[0426] R(4) is C_(p)F_(2p+1);

[0427] p is 1, 2 or 3, if n is zero or 1;

[0428] or

[0429] R(4) is (C₃-C₁₂)-cycloalkyl, phenyl, pyridyl, quinolyl orisoquinolyl,

[0430] where the aromatic and heteroaromatic ring systems areunsubstituted or substituted by a substituent selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and

[0431] NR(5)R(6);

[0432] R(5) and R(6)

[0433] are hydrogen or (C₁-C₄)-alkyl;

[0434] or one of the substituents R(1), R(2) or R(3)

[0435] is —C≡CR(5) or —C[R(6)]═CR(5);

[0436] R(5) is phenyl,

[0437] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy,hydroxyl, amino, methylamino and dimethylamino, (C₁-C₉)-heteroaryl,

[0438] which is unsubstituted or substituted as phenyl,

[0439] or

[0440] R(5) is (C₁-C6)-alkyl,

[0441] which is unsubstituted or substituted by 1-3 OH;

[0442] or

[0443] R(5) is (C₃-C₈)-cycloalkyl,

[0444] R(6) is hydrogen or methyl;

[0445] and their pharmacologically acceptable salts;

[0446] 93/F 153—EP-A 627 413, NZ 260 660)

[0447] o) benzoylguanidines of the formula I

[0448] in which:

[0449] R(1) is hydrogen, F, Cl, Br, I, —NO₂, —C≡N,X_(o)—(CH₂)_(p)—(CF₂)_(q)—CF₃, R(5)—SO_(m), R(6)—CO— or R(6)R(7)N—SO₂—,where

[0450] X is oxygen, S or NR(14);

[0451] m is zero, 1 or 2;

[0452] o is zero or 1;

[0453] p is zero, 1 or 2;

[0454] q is zero, 1, 2, 3, 4, 5 or 6;

[0455] R(5) and R(6)

[0456] are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(8) or CF₃;

[0457] n is zero, 1, 2, 3 or 4;

[0458] R(8) is (C₃-C₇)-cycloalkyl or phenyl,

[0459] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10);

[0460] R(9) and R(10)

[0461]  are H or C₁-C₄-alkyl;

[0462] or

[0463] R(6) is H;

[0464] R(7) is H or (C₁-C₄)-alkyl;

[0465] or

[0466] R(6) and R(7)

[0467] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0468] Y is oxygen, —S— or —NR(12)—;

[0469] R(11) and R(12)

[0470]  are hydrogen or (C₁-C₃)-alkyl;

[0471] h is zero or 1;

[0472] i, j and k

[0473]  independently are zero, 1, 2, 3 or 4;

[0474] but where h, i and k are not simultaneously zero,

[0475] R(3) is defined as R(1), or is (C₁-C₆)-alkyl or —X—R(13);

[0476] X is oxygen, S or NR(14);

[0477] R(14) is H or (C₁-C₃)-alkyl;

[0478] R(13) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(b)H_(2b)—R(15);

[0479] b is zero, 1, 2, 3 or 4;

[0480] or

[0481] R(13) and R(14)

[0482] together are 4 or 5 methylene groups, where one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0483] R(15) is phenyl,

[0484] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10);

[0485] R(9) and R(10)

[0486]  are H or (C₁-C₄)-alkyl;

[0487] R(4) is hydrogen, —OR(16) or —NR(16)R(17);

[0488] R(16) and R(17)

[0489] independently are hydrogen or (C₁-C₃)-alkyl;

[0490] and their pharmaceutically tolerable salts;

[0491] (HOE 93/F 154—EP-A 628 543, NZ 260 681)

[0492] p) benzoylguanidines of the formula I

[0493] in which:

[0494] R(1) is R(6)—CO or R(7)R(8)N—CO;

[0495] R(6) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(n)H_(2n)—R(9);

[0496] n is zero, 1, 2, 3 or 4;

[0497] R(9) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0498] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(10)R(11);

[0499] R(10) and R(11)

[0500]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0501] R(7) is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenylor —C_(n)H_(2n)—R(12);

[0502] n is zero, 1, 2, 3 or 4;

[0503] R(12) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0504] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(13)R(14);

[0505] R(13) and R(14)

[0506]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0507] R(8) is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0508] or

[0509] R(7) and R(8)

[0510] together are 4 or 5 methylene groups, of which one CH2 group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0511] R(2) is defined as R(1), or is H, F, Cl, Br, I, CN, NO₂,(C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C3-C₈)-alkenyl or—C_(n)H_(2n)R(15);

[0512] n is zero, 1, 2, 3 or 4;

[0513] R(15) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0514] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and

[0515] NR(16)R(17);

[0516] R(16) and R(17)

[0517]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0518] or

[0519] R(2) is (C₁-C₉)-heteroaryl,

[0520] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[0521] or

[0522] R(2) is SR(18), —OR(18), —NR(18)R(19), —CR(18)R(19)R(20);

[0523] R(18) is —C_(a)H_(2a)—(C₁-C₉)-heteroaryl,

[0524] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[0525] a is zero, 1 or 2;

[0526] R(19) and R(20)

[0527] independently of one another are defined as R(18) or arehydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0528] or

[0529] R(2) is R(21)—SO_(m) or R(22)R(23)N—SO₂—;

[0530] m is 1 or 2;

[0531] R(21) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl,—C_(n)H_(2n),—R(24),

[0532] n is zero, 1, 2, 3 or 4;

[0533] R(24) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0534] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(27)R(28);

[0535] R(27) and R(28)

[0536]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0537] R(22) is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl, —C_(n)H_(2n)—R(29);

[0538] n is zero, 1, 2, 3 or 4;

[0539] R(29) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0540] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(30)R(31);

[0541] R(30) and R(31)

[0542]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0543] R(23) is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0544] or

[0545] R(22) and R(23)

[0546] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0547] or

[0548] R(2) is R(33)X—;

[0549] X is oxygen, S, NR(34), (D═O)A—, NR(34)C═MN^((*))R(35)—;

[0550] M is oxygen or S;

[0551] A is oxygen or NR(34);

[0552] D is C or SO;

[0553] R(33) is (C₁-C₈),alkyl (C₃-C₈)-alkenyl, (CH₂)_(b)C_(d)F_(2d+1),—C_(n)H_(2n)—R(36),

[0554] b is zero or 1;

[0555] d is 1, 2, 3, 4, 5, 6 or 7;

[0556] n is zero, 1, 2, 3 or 4;

[0557] R(36) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0558] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(37)R(38);

[0559] R(37) and R(38)

[0560]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0561] R(34) is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0562] R(35) is defined as R(33);

[0563] or

[0564] R(33) and R(34)

[0565] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0566]  where A and N^((*)) are bonded to the phenyl nucleus of thebenzoylguanidine parent structure;

[0567] or

[0568] R(2) is —SR(40), —OR(40), —NHR(40), —NR(40)R(41), —CHR(40)R(42),—C[R(42)R(43)OH], —C≡CR(45), —CR(46)═CHR(45),—[CR(47)R(48)]_(u)—(CO)—[CR(49)R(50)]_(v)—R(44);

[0569] R(40), R(41)

[0570] identically or differently are—(CH₂)_(p)—(CHOH)_(q)—(CH₂)_(r)—(CHOH)_(t)—R(51) or—(CH₂)_(p)—O—(CH₂—CH₂O)_(q)—R(51);

[0571] R(51) is hydrogen or methyl;

[0572] u is 1, 2, 3 or 4;

[0573] v is zero, 1, 2, 3 or 4;

[0574] p, q, r

[0575] identically or differently are zero, 1, 2, 3 or 4;

[0576] t is 1, 2, 3 or 4;

[0577] R(42) and R(43)

[0578] identically or differently are hydrogen or (C₁-C₆)-alkyl;

[0579] or

[0580] R(42) and R(43)

[0581] together with the carbon atom carrying them form a(C₃-C₈)-cycloalkyl;

[0582] R(44) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(e)H_(2e)—R(45);

[0583] e is zero, 1, 2, 3 or 4;

[0584] R(45) is phenyl,

[0585] which is unsubstituted or substituted by 1-3 substituents fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(52)R(53)where

[0586]  R(52) and R(53) are H or (C₁-C₄)-alkyl, or

[0587] R(45) is (C₁-C₉)-heteroaryl,

[0588] which is unsubstituted or substituted as phenyl;

[0589] or

[0590] R(45) is (C₁-C₆)-alkyl,

[0591] which is unsubstituted or substituted by 1-3 OH;

[0592] R(46), R(47), R(48), R(49) and R(50)

[0593] are hydrogen or methyl;

[0594] or

[0595] R(2) is R(55)—NH—SO₂—;

[0596] R(55) is R(56)R(57)N—(C═Y)—;

[0597] Y is oxygen, S or N—R(58);

[0598] R(56) and R(57)

[0599] identically or differently are H, (C₁-C₈)-alkyl, (C₃-C₆)-alkenylor —C_(f)H_(2f)—HR(59);

[0600] f is zero, 1, 2, 3 or 4;

[0601] R(59) is (C₅-C₇)-cycloalkyl or phenyl,

[0602]  which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methoxy and(C₁-C₄)-alkyl;

[0603] or

[0604] R(⁵⁶) and R(57)

[0605] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0606] R(58) is defined as R(56) or is amidine;

[0607] R(3), R(4) and R(5)

[0608] independently of one another are defined as R(1) or R(2);

[0609] and their pharmaceutically tolerable salts;

[0610] (HOE 93/F 220—EP-A 640 593, NZ 264 117)

[0611] q) benzoylguanidines of the formula I

[0612] in which:

[0613] R(1) is hydrogen, F, Cl, Br, I, —NO², —C≡N,—X_(o)—(CH₂)_(p)—(CF₂)_(q)—CF₃,

[0614] R(5)—SO_(m)—, R(6)—CO—, R(6)R(7)N—CO— or R(6)R(7)N—SO₂—;

[0615] X is oxygen, —S— or NR(14);

[0616] m is zero, 1 or 2;

[0617] o is zero or 1;

[0618] p is zero, 1 or 2;

[0619] q is zero, 1, 2, 3, 4, 5 or 6;

[0620] R(5) and R(6)

[0621] are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(8) or CF₃;

[0622] n is zero, 1, 2, 3 or 4;

[0623] R(8) is (C₃-C₇)-cycloalkyl, phenyl,

[0624] which is not substituted or is substituted by 1 to 3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10);

[0625] R(9) and R(10)

[0626]  are H or (C₁-C₄)-alkyl;

[0627] or

[0628] R(6) is hydrogen;

[0629] R(7) is hydrogen or (C₁-C₄)-alkyl;

[0630] or

[0631] R(6) and R(7)

[0632] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0633] R(2) is

[0634] R(11) is (C₁-C₉)-heteroaryl,

[0635] which is linked via C or N and which is unsubstituted orsubstituted by 1 to 3 substituents selected from the group consisting ofF, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino, dimethylaminoand benzyl;

[0636] Y is oxygen, —S— or NR(12);

[0637] R(12) is H or (C₁-C₄)-alkyl;

[0638] R(3) is defined as R(1);

[0639] or

[0640] R(3) is (C₁-C₆)-alkyl or —X—R(13);

[0641] X is oxygen, —S— or NR(14);

[0642] R(14) is H or (C₁-C₃)-alkyl;

[0643] R(13) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(b)H_(2b)—R(15);

[0644] b is zero, 1, 2, 3 or 4;

[0645] or

[0646] R(13) and R(14)

[0647] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0648] R(15) is phenyl,

[0649] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10);

[0650] R(9) and R(10)

[0651]  are H or (C₁-C₄)-alkyl;

[0652] R(4) is hydrogen, —OR(16), —NR(16)R(17) or C_(r)F_(2r+1);

[0653] R(16) and R(17)

[0654] independently are hydrogen or (C₁-C₃)-alkyl;

[0655] r is 1, 2, 3 or 4;

[0656] and their pharmaceutically tolerable salts;

[0657] (HOE 93/F 223K—EP 639 573, NZ 264 130)

[0658] r) benzo-fused 5-membered ring heterocycles of the formula I

[0659] in which:

[0660] X is N or CR(6);

[0661] Y is oxygen, S or NR(7);

[0662] A, B together are a bond

[0663] or

[0664] A, B are both hydrogen, if X is CR(6) and Y is NR(7)simultaneously;

[0665] one of the substituents R(1) to R(6) is a —CO—N═C(NH₂)₂ group;

[0666] the other substituents R(1) to R(6) in each case

[0667] are hydrogen, F, Cl, Br, I or (C₁-C₆)-alkyl;

[0668] up to two of the other substituents R(1) to R(6)

[0669] are CN, NO₂, N₃, (C₁-C₄)-alkyloxy or CF₃;

[0670] up to one of the other substituents

[0671] is R(8)—C_(n)H_(2n)—Z—;

[0672] n is zero to 10;

[0673] where the alkylene chain —C_(n)H_(2n)— is straight-chain orbranched and where one carbon atom can be replaced by an oxygen orsulfur atom or by a nitrogen atom;

[0674] R(8) is hydrogen, (C₂-C₆)-alkenyl or (C₃-C₁₀)-cycloalkyl,

[0675] which is unsubstituted or substituted by 1 to 4 methyl groups oran OH group, or can contain an ethylene group —CH═CH—, and in which onemethylene group can be replaced by an oxygen or sulfur atom or by anitrogen atom;

[0676] or

[0677] R(8) is phenyl,

[0678] which is unsubstituted or substituted by 1 to 3 substituentsselected from the group consisting of F, Cl, Br, I, CF₃, CH₃—S(O)_(s)—or R(9)—W_(y)—;

[0679] s is zero, 1 or 2;

[0680] R(9) is H, methyl, ethyl,

[0681] W is oxygen or NR(10);

[0682] R(10) is H or methyl;

[0683] y is zero or 1;

[0684] or

[0685] R(8) is C_(m)F_(2m+1);

[0686] m is 1 to 3;

[0687] or

[0688] R(8) is 1- or 2-naphthyl, pyridyl, quinolyl or isoquinolyl;

[0689] Z is —CO—, —CH₂— or —[CR(11)(OH)]_(q)—;

[0690] q is 1, 2 or 3;

[0691] R(11) is H or methyl;

[0692] or

[0693] Z is oxygen or —NR(12)—;

[0694] R(12) is H or methyl;

[0695] or

[0696] Z is —S(O)_(s)—;

[0697] s is zero, 1 or 2;

[0698] or

[0699] Z is —SO₂—NR(13)—;

[0700] R(13) is H or (C₁-C₄)-alkyl;

[0701] R(7) is hydrogen, (C₁-C₁₀)-alkyl, (C₂-C₁₀)-alkenyl orR(8)—C_(n)H_(2n)—;

[0702] and their pharmaceutically tolerable salts;

[0703] (HOE 93/F 236—EP-A 638 548, NZ 264 216)

[0704] s) benzoylguanidines of the formula I

[0705] in which:

[0706] R(1), R(3) or R(4)

[0707] is —NR(6) C═X NR(7)R(8);

[0708] X is oxygen or S;

[0709] R(6) is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(n)H_(2n)—R(9);

[0710] n is zero, 1, 2, 3 or 4;

[0711] R(9) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0712]  where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and

[0713]  NR(10)R(11);

[0714]  R(10) and R(11)

[0715]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0716] R(7) is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(o)H_(2o)—R(12);

[0717] o is zero, 1, 2, 3 or 4;

[0718] R(12) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0719]  where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(13)R(14);

[0720]  R(13) and R(14)

[0721]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0722] R(8) is defined as R(7);

[0723] or

[0724] R(7) and R(8)

[0725] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0726] the remaining substituents R(2), R(3), R(4), R(5) or R(1), R(2),R(4), R(5) or R(1), R(2), R(3), R(5) in each case

[0727] independently of one another are hydrogen, F, Cl, Br, I,—O_(ta)(C₁-C₈)-alkyl, —O_(tb)(C₃-C₈)-alkenyl,

[0728] —O_(tc)(CH₂)_(b)C_(d)F_(2d+1), —O_(td)C_(p)H_(2p)R(18),

[0729] or up to 2 groups CN, NO₂, NR(16)R(17),

[0730] b is zero or 1;

[0731] d is 1, 2 , 3, 4, 5, 6 or 7;

[0732] ta is zero or 1;

[0733] tb is zero or 1;

[0734] tc is zero or 1;

[0735] td is zero or 1;

[0736] p is zero, 1, 2, 3 or 4;

[0737] R(18) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0738] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(19)R(20);

[0739] R(19) and R(20)

[0740] are hydrogen or (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0741] R(16) is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl, —C_(q)H_(2q)—R(21),

[0742] q is zero, 1, 2, 3 or 4;

[0743] R(21) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0744] where the aromatics are not substituted or are substituted by 1-3substituents from the group F, Cl, CF₃, methyl, methoxy or NR(22)R(23),

[0745] R(22) and R(23) are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl;

[0746] R(17) is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl, —C_(r)H_(2r)—R(24);

[0747] r is zero, 1, 2, 3 or 4;

[0748] R(24) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0749] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(25)R(26);

[0750] R(25) and R(26)

[0751]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0752] or

[0753] R(16) and R(17)

[0754] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0755] and their pharmaceutically tolerable salts;

[0756] (HOE 93/F 249—EP-A 640 587, NZ 264 282)

[0757] t) diacyl-substituted guanidines of the formula I

[0758] in which:

[0759] X(1) and X(2) are

[0760] T1 is zero, 1, 2, 3 or 4;

[0761] R(A) and R(B)

[0762] independently of one another are hydrogen, F, Cl, Br, I, CN,OR(106), (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl,O_(zk)(CH₂)_(zl)C_(zm)F_(2zm+1), NR(107)R(108), phenyl or benzyl,

[0763] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(109)R(110);

[0764] R(109) and R(110)

[0765]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0766] zl is zero, 1, 2, 3 or 4;

[0767] zk is zero or 1;

[0768] zm is 1, 2, 3, 4, 5, 6, 7 or 8;

[0769] R(106)

[0770] is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl, (C₃-C₈)-cycloalkyl, phenyl or benzyl,

[0771]  where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and

[0772]  NR(111)R(112);

[0773]  R(111) and R(112)

[0774]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)perfluoroalkyl;

[0775] R(107) and R(108)

[0776] independently of one another are defined as R(106),

[0777] or

[0778] R(107) and R(108)

[0779] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0780] or

[0781] X(1) and X(2) are

[0782] T2a and T2b

[0783] independently of one another are zero, 1 or 2;

[0784] where the double bond can have the (E)- or (Z)-configuration;

[0785] or

[0786] X(1) and X(2) are

[0787] T3 is zero, 1 or 2;

[0788] U, YY and Z

[0789] independently of one another are C or N,

[0790] where U, YY, Z can carry the following number of substituents:Bonded in the ring to Number of permitted U, YY or Z a double bondsubstituents C yes 1 C no 2 N yes 0 N no 1

[0791] R(D) is hydrogen, (C₁-C₈)-alkyl or (C₁-C₈)-perfluoroalkyl,

[0792] R(U1), R(U2), R(Y1), R(Y2), R(Z1), R(Z2)

[0793] independently of one another are hydrogen, F, Cl, Br, I, CN,OR(114), (C₁-C₈)-alkyl, (C₃-C8)-cycloalkyl,O_(zka)(CH₂)_(zla)C_(zma)F_(2zma+1),

[0794] NR(115)R(116), phenyl or benzyl,

[0795] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy, NR(117)R(118),

[0796] R(117) and R(118)

[0797]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl,

[0798] zka is zero or 1;

[0799] zla is zero, 1, 2, 3 or 4;

[0800] zma is 1, 2, 3, 4, 5, 6, 7 or 8;

[0801] R(114)

[0802] is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl, (C₃-C₈)-cycloalkyl, phenyl or benzyl,

[0803]  where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and

[0804]  NR(119)R(120);

[0805]  R(119) and R(120)

[0806]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0807] R(115) and R(116) independently of one another are defined asR(114);

[0808] or

[0809] R(115) and R(116)

[0810] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[0811] but where the constitution of U is nitrogen (N), YY is nitrogen(N) and Z is carbon (C) is excluded,

[0812] R(101), R(102), R(103), R(104) and R(105)

[0813] independently of one another are hydrogen, F, Cl, Br, I, —C≡N,

[0814] X_(zoa)—(CH₂)_(zpa)—(C_(zqa)F_(2zqa+1)), R(110a)—SO_(zbm),R(110b)R(110c)N—CO,

[0815] R(111a)—CO— or R(112a)R(113a)N—SO₂—,

[0816] where the perfluoroalkyl group is straight-chain or branched,

[0817] X is oxygen, S or NR(114a);

[0818] R(114a)

[0819]  is H or (C₁-C₃)-alkyl;

[0820] zoa is zero or 1;

[0821] zbm is zero, 1 or 2;

[0822] zpa is zero, 1, 2, 3 or 4;

[0823] zqa is 1, 2, 3, 4, 5, 6, 7 or 8;

[0824] R(110a), R(110b), R(111a) and R(112a)

[0825] independently of one another are (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl,—C_(n)H_(2zn)—R(115a) or (C₁-C₈)-perfluoroalkyl;

[0826] zn is zero, 1, 2, 3 or 4;

[0827] R(115a)

[0828]  is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0829]  where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(116a)R(117a);

[0830]  R(116a) and R(117a)

[0831]  are hydrogen, (C₁-C₄)-perfluoroalkyl or (C₁-C₄)-alkyl;

[0832] or

[0833] R(110b), R(111a) and R(112a)

[0834] are hydrogen;

[0835] R(110c) and R(113a)

[0836] independently are hydrogen, (C₁-C₄)-perfluoroalkyl or(C₁-C₄)-alkyl;

[0837] or

[0838] R(110b) and R(110c) and R(112a) and R(113a)

[0839] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[0840] or

[0841] R(101), R(102), R(103), R(104), R(105)

[0842] independently of one another are (C₁-C₈)-alkyl,—C_(zal)H_(2zal)R(118a) or (C₃-C₈)-alkenyl,

[0843] zal is zero, 1, 2, 3 or 4;

[0844] R(118a)

[0845] is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0846]  where the aromatics are not substituted or are substituted by1-3 substituents from the group consisting of F, Cl, CF₃, methyl,methoxy or

[0847]  NR(119a)R(119b);

[0848]  R(119a) and R(119b)

[0849]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0850] or

[0851] R(101), R(102), R(103), R(104), R(105)

[0852] independently of one another are (C₁-C₉)-heteroaryl,

[0853] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents from the group consisting of F, Cl, CF₃,CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[0854] or

[0855] R(101), R(102), R(103), R(104), R(105)

[0856] independently of one another are —C≡C—R(193);

[0857] R(193)

[0858] is phenyl which is not substituted or is substituted by 1-3substituents from the group consisting of F, Cl, CF₃, methyl, methoxy orNR(194)R(195);

[0859] R(194) and R(195)

[0860]  are hydrogen or CH₃;

[0861] or

[0862] R(101), R(102), R(103), R(104), R(105)

[0863] independently of one another are

[0864] —Y-para-C₆H₄—(CO)_(zh)—(CHOH)_(zi)—(CH2)_(zj)—(CHOH)_(zk)—R(123),

[0865]—Y-meta-C₆H₄—(CO)_(zad)—(CHOH)_(zae)—(CH₂)_(zaf)—(CHOH)_(zag)—R(124)

[0866] or

[0867]—Y-ortho-C₆H₄—(CO)_(zah)—(CHOH)_(zao)—(CH₂)_(zap)—(CHOH)_(zak)—R(125);

[0868] Y is oxygen, —S— or —NR(122d)—;

[0869] zh, zad, zah

[0870] independently are zero or 1;

[0871] zi, zj, zk, zae, zaf, zag, zao, zap and zak

[0872] independently are zero, 1, 2, 3 or 4;

[0873] but where in each case

[0874] zh, zi and zk are not simultaneously zero,

[0875] zad, zae and zag are not simultaneously zero, and

[0876] zah, zao and zak are not simultaneously zero,

[0877] R(123), R(124), R(125) and R(122d)

[0878] independently are hydrogen or (C₁-C₃)-alkyl;

[0879] or

[0880] R(101), R(102), R(103), R(104) and R(105)

[0881] independently of one another are SR(129), —OR(130),

[0882] —NR(131)R(132) or —CR(133)R(134)R(135);

[0883] R(129), R(130), R(131) and R(133)

[0884] independently are —C_(zab)H_(2zab)—(C₁-C₉)-heteroaryl,

[0885]  which is unsubstituted or substituted by 1-3 substituents fromthe group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino;

[0886] zab is zero, 1 or 2;

[0887] R(132), R(134) and R(135)

[0888] independently of one another are defined as R(129) or arehydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0889] or

[0890] R(101), R(102), R(103), R(104) and R(105)

[0891] independently of one another are —W-para-(C₆H₄)—R(196),—W-meta-(C₆H₄)—R(197) or —W-ortho-(C₆H₄)—R(198);

[0892] R(196), R(197) and R(198)

[0893] independently are (C₁-C₉)-heteroaryl,

[0894]  which is linked via C or N and which is unsubstituted orsubstituted by 1 to 3 substituents from the group consisting of F, Cl,CF₃, CH₃, methoxy, hydroxyl, amino, methylamino, dimethylamino andbenzyl;

[0895] W is oxygen, S or NR(136)—;

[0896] R(136)

[0897]  is hydrogen or (C₁-C₄)-alkyl;

[0898] or

[0899] R(101), R(102), R(103), R(104) and R(105)

[0900] independently of one another are R(146)X(1a)—;

[0901] X(1a)

[0902] is oxygen, S, NR(147), (D═O)A—, NR(148)C═MN^((*))R(149)—;

[0903] M is oxygen or sulfur;

[0904] A is oxygen or NR(150);

[0905] D is C or SO;

[0906] R(146)

[0907] is (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, (CH₂)_(zbz)C_(zdz)F_(2zdz+1)or —C_(zxa)H_(2zxa)—

[0908] R(151);

[0909] zbz is zero or 1;

[0910] zdz is 1, 2, 3, 4, 5, 6 or 7;

[0911] zxa is zero, 1, 2, 3 or 4;

[0912] R(151)

[0913]  is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[0914]  where the aromatics are not substituted or are substituted by1-3 substituents from the group consisting of F, Cl, CF₃, methyl,methoxy and

[0915]  NR(152)R(153);

[0916]  R(152) and R(153)

[0917]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[0918] R(147), R(148) and R(150)

[0919] independently are hydrogen, (C₁-C₄)-alkyl,(C₁-C₄)-perfluoroalkyl;

[0920] R(149) is defined as R(146),

[0921] or

[0922] R(146) and R(147), or R(146) and R(148)

[0923] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[0924]  where A and N^((*)) are bonded to the phenyl nucleus of thealkanoyl parent structure;

[0925] or

[0926] R(101), R(102), R(103), R(104) and R(105)

[0927] independently of one another are —SR(164), —OR(165), —NHR(166),

[0928] —NR(167)R(168), —CHR(169)R(170), —CR(154)R(155)OH,

[0929] —C≡CR(156), —CR(158)═CR(157) or

[0930] —[CR(159)R(160)]_(zu)—(C═O)—[CR(161)R(162)]_(zv)—R(163);

[0931] R(164), R(165), R(166), R(167), R(169)

[0932] identically or differently are—(CH₂)_(zy)—(CHOH)_(zz)—(CH₂)_(zaa)—(CHOH)_(zt)—R(171) or—(CH₂)_(zab)—O—(CH₂—CH₂O)_(zac)—R(172);

[0933] R(171) and R(172)

[0934]  are hydrogen or methyl;

[0935] zu is 1, 2, 3 or 4;

[0936] zv is zero, 1, 2, 3 or 4;

[0937] zy, zz, zaa, zab, zac

[0938]  identically or differently are zero, 1, 2, 3 or 4;

[0939]  zt is 1, 2, 3 or 4;

[0940] R(168), R(170), R(154), R(155)

[0941] identically or differently are hydrogen or (C₁-C₆)-alkyl,

[0942] or

[0943] R(169) and R(170), or R(154) and R(155) together with the carbonatom carrying them are a (C₃-C₈)-cycloalkyl;

[0944] R(163)

[0945] is hydrogen, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or

[0946] —C_(zeb)H_(2zeb)—R(173);

[0947] zeb is zero, 1, 2, 3 or 4;

[0948] R(156), R(157) and R(173)

[0949]  independently are phenyl which is unsubstituted or issubstituted by 1-3 substituents from the group consisting of F, Cl, CF₃,methyl, methoxy and

[0950] NR(174)R(175);

[0951] R(174) and R(175)

[0952]  are hydrogen or (C₁-C₄)-alkyl;

[0953] or

[0954] R(156), R(157) and R(173)

[0955] independently are (C₁-C₉)-heteroaryl,

[0956]  which is unsubstituted or substituted as phenyl;

[0957] R(158), R(159), R(160), R(161) and R(162)

[0958] are hydrogen or methyl,

[0959] or

[0960] R(101), R(102), R(103), R(104), R(105)

[0961] independently of one another are R(176)—NH—SO₂—;

[0962] R(176)

[0963] is R(177)R(178)N—(C═Y′)—;

[0964] Y′ is oxygen, S or N—R(179);

[0965] R(177) and R(178)

[0966]  identically or differently are hydrogen, (C₁-C₈)-alkyl,(C₃-C6)-alkenyl or —C_(zfa)H_(2zfa)—R(180);

[0967]  zfa is zero, 1, 2, 3 or 4;

[0968]  R(180)

[0969]  is (C₅-C₇)-cycloalkyl or phenyl,

[0970]  which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methoxy

[0971]  or (C₁-C₄)-alkyl;

[0972] or

[0973] R(177) and R(178)

[0974]  together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[0975] R(179)

[0976]  is defined as R(177) or is amidine,

[0977] or

[0978] R(101), R(102), R(103), R(104), R(105)

[0979] independently of one another are NR(184a)R(185), OR(184b),

[0980] SR(184c) or —C_(znx)H_(2znx)—R(184d);

[0981] znx is zero, 1, 2, 3 or 4;

[0982] R(184d)

[0983] is (C₃-C₇)-cycloalkyl or phenyl,

[0984]  which is not substituted or is substituted by 1-3 substituentsfrom the group consisting of F, Cl, CF₃, methyl, methoxy andNR(116k)R(117k);

[0985]  R(116k) and R(117k)

[0986]  are hydrogen or C₁-C₄-alkyl;

[0987] R(184a), R(184b), R(184c), R(185)

[0988] independently of one another are hydrogen, (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl or (CH₂)_(zao)—R(184g);

[0989] zao is zero, 1, 2, 3 or 4;

[0990] 184g

[0991]  is (C₃-C₇)-cycloalkyl or phenyl,

[0992]  which is not substituted or is substituted by 1-3 substituentsfrom the group consisting of F, Cl, CF₃, methyl, methoxy andNR(184u)R(184v);

[0993]  R(184u) and R(184v)

[0994]  are hydrogen or C₁-C₄-alkyl;

[0995] or

[0996] R(184a) and R(185)

[0997] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[0998] and their pharmaceutically tolerable salts;

[0999] (HOE 93/F 254—EP-A 640 588, NZ 264 307)

[1000] u) benzoylguanidines of the formula I

[1001] in which:

[1002] R(1) is H, F, Cl, Br, I, CN, NO₂, (C₁-C₈)-alkyl,(C₃-C₈)-cycloalkyl or

[1003] X_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃;

[1004] X is oxygen, S or NR(5);

[1005] a is zero or 1;

[1006] b is zero, 1 or 2;

[1007] c is zero, 1, 2 or 3;

[1008] R(5) is H, (C₁-C₄)-alkyl or —C_(d)H_(2d)R(6);

[1009] d is zero, 1, 2, 3 or 4;

[1010] R(6) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1011]  where the aromatics are not substituted or are substituted by 1to 3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(7)R(8);

[1012]  R(7) and R(8)

[1013]  independently are H or (C₁-C4)-alkyl;

[1014] or

[1015] R(1) is —SR(10), —OR(10) or —CR(10)R(11)R(12);

[1016] R(10) is —C_(f)H_(2f)—(C₃-C₈)-cycloalkyl, —(C₁-C₉)-heteroaryl orphenyl,

[1017] where the aromatic systems are unsubstituted or substituted by 1to 3 substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino;

[1018] f is zero, 1 or 2;

[1019] R(11) and R(12)

[1020] independently of one another are defined as R(10) or are hydrogenor (C₁-C₄)-alkyl;

[1021] or

[1022] R(1) is phenyl, naphthyl, biphenylyl or (C₁-C₉)-heteroaryl,

[1023] the latter linked via C or N,

[1024] and which are unsubstituted or substituted by 1 to 3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[1025] or

[1026] R(1) is —SR(13), —OR(13), —NHR(13), —NR(13)R(14), —CHR(13)R(15),—C[R(15)R(16)]OH, —C≡CR(18), —C[R(19)]═CR(18),—[CR(20)R(21)]_(k)—(CO)—[CR(22)R(23)R(24)]_(l)

[1027] R(13) and R(14)

[1028] identically or differently are—(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(j)—R(17),

[1029] R(17) is hydrogen or methyl;

[1030] —(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(24),

[1031] g, h, i

[1032] identically or differently are zero, 1, 2, 3 or 4;

[1033] j is 1, 2, 3 or 4;

[1034] R(15) and R(16)

[1035] identically or differently are hydrogen, (C₁-C₆)-alkyl ortogether with the carbon atom carrying them are a (C₃-C₈)-cycloalkyl;

[1036] R(18) is phenyl,

[1037] which is unsubstituted or substituted by 1 to 3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(25)R(26);

[1038] R(25) and R(26)

[1039] are H or (C₁-C₄)-alkyl;

[1040] or

[1041] R(18) is (C₁-C₉)-heteroaryl,

[1042] which is unsubstituted or substituted as phenyl;

[1043] or

[1044] R(18) is (C₁-C₆)-alkyl,

[1045] which is unsubstituted or substituted by 1 to 3 OH;

[1046] or

[1047] R(18) is (C₃-C₈)-cycloalkyl;

[1048] R(19), R(20), R(21), R(22) and R(23)

[1049] are hydrogen or methyl;

[1050] k is zero, 1, 2, 3 or 4;

[1051] l is zero, 1, 2, 3or 4;

[1052] R(24) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(m)H_(2m)—R(18);

[1053] m is 1, 2, 3 or 4;

[1054] R(2) and R(3)

[1055] independently of one another are defined as R(1);

[1056] R(4) is (C₁-C₃)-alkyl, F, Cl, Br, I, CN or—(CH₂)_(n)—(CF₂)_(o)—CF₃;

[1057] n is zero or 1;

[1058] o is zero, 1 or 2;

[1059] and their pharmaceutically tolerable salts;

[1060] (HOE 93/F 436—EP-A 659 748), NZ 270 264)

[1061] v) acylguanidines of the formula I

[1062] in which:

[1063] X is carbonyl, sulfonyl,

[1064] R(1) is H, (C₁-C₈)-alkyl,

[1065] unsubstituted or substituted by hydroxyl, (C₃-C₈)-cycloalkyl,phenyl,

[1066] which is unsubstituted or substituted by 1-3 substituents fromthe group F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino ordimethylamino,

[1067] R(2) is H, (C₁-C₄)-alkyl,

[1068] and their pharmaceutically tolerable salts;

[1069] (HOE 94/F 014 K—EP-A 666 252, NZ 270 370)

[1070] w) phenyl-substituted alkylcarboxylic acid guanidides, carryingperfluoroalkyl groups, of the formula I

[1071] in which:

[1072] R(A) is hydrogen, F, Cl, Br, I, CN, OR(6), (C₁-C₈)-alkyl,(C₃-C₈)-cycloalkyl, O_(r)(CH₂)_(a)C_(b)F_(2b+1) or NR(7)R(8);

[1073] r is zero or 1;

[1074] a is zero, 1, 2, 3 or 4;

[1075] b is 1, 2, 3, 4, 5, 6, 7 or 8;

[1076] R(6) is hydrogen, (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl,(C₃-C₈)-cycloalkyl, phenyl or benzyl,

[1077] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and

[1078] NR(9)R(10);

[1079] R(9) and R(10)

[1080] are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1081] R(7) and R(8)

[1082] independently of one another are defined as R(6);

[1083] R(B) independently is defined as R(A);

[1084] X is 1, 2 or 3;

[1085] R(1) is hydrogen, (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl,—O_(t)(CH₂)_(d)C_(e)F_(2e+1), F, Cl, Br, I or CN;

[1086] t is zero or 1;

[1087] d is zero, 1, 2, 3 or 4;

[1088] e is 1, 2, 3, 4, 5, 6, 7 or 8;

[1089] R(2), R(3), R(4) and R(5)

[1090] independently of one another are defined as R(1);

[1091] but with the condition that at least one of the substituentsR(1), R(2), R(3), R(4), R(5), R(A) and R(B) is an—O_(t)(CH₂)_(d)C_(e)F_(2e+1) or an O_(r)(CH₂)_(a)C_(b)F_(2b+1) group,

[1092] and their pharmaceutically tolerable salts;

[1093] (HOE 94/F 094—EP-A 676 395, NZ 270 894)

[1094] x) heteroaroylguanidines of the formula I

[1095] in which:

[1096] HA is SO_(m), O or NR(5);

[1097] m is zero, 1 or 2;

[1098] R(5) is hydrogen, (C₁-C₈)-alkyl or —C_(am)H_(2am)R(81);

[1099] am is zero, 1 or 2;

[1100] R(81) is (C₃-C₈)-cycloalkyl or phenyl,

[1101] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(82)R(83);

[1102] R(82) and R(83)

[1103]  is H or CH₃;

[1104] or

[1105] R(81) is (C₁-C₉)-heteroaryl,

[1106] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[1107] one of the two substituents R(1) and R(2)

[1108] is —CO—N═C(NH₂)₂;

[1109] and the other in each case

[1110] is hydrogen, F, Cl, Br, I, (C₁-C₃)-alkyl, —OR(6), C_(r)F_(2r+1),—CO—N═C(NH₂)₂ or —NR(6)R(7);

[1111] R(6) and R(7)

[1112] independently are hydrogen or (C₁-C₃)-alkyl;

[1113] r is 1, 2, 3 or 4;

[1114] R(3) and R(4)

[1115] independently of one another are hydrogen, F, Cl, Br, I, —C≡N,X—(CH₂)_(p)—(C_(q)—F_(2q+1)), R(8)—SO_(bm), R(9)R(10)N—CO, R(11)—CO — or

[1116] R(12)R(13)N—SO₂—,

[1117] where the perfluoroalkyl group is straight-chain or branched,

[1118] X is oxygen, S or NR(14);

[1119] R(14) is H or (C₁-C₃)-alkyl;

[1120] bm is zero, 1 or 2;

[1121] p is zero, 1 or 2;

[1122] q is zero, 1, 2, 3, 4, 5 or 6;

[1123] R(8), R(9), R(11) and R(12)

[1124] independently are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl,—C_(n)H_(2n)—R(15), CF₃;

[1125] n is zero, 1, 2, 3 or 4;

[1126] R(15) is (C₃-C₇)-cycloalkyl or phenyl,

[1127] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy orNR(16)R(17);

[1128] R(16) and R(17)

[1129]  are H or C₁-C₄-alkyl;

[1130] or

[1131] R(9), R(11) and R(12)

[1132] are H;

[1133] R(10) and R(13)

[1134] independently are H or (C₁-C₄)-alkyl;

[1135] or

[1136] R(9) and R(10), and R(12) and R(13)

[1137] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl,

[1138] or

[1139] R(3) and R(4)

[1140] independently of one another are (C₁-C₈)-alkyl or—C_(al)H_(2al)R(18);

[1141] al is zero, 1 or 2;

[1142] R(18) is (C₃-C₈)-cycloalkyl or phenyl;

[1143] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(19)R(20);

[1144] R(19) and R(20)

[1145]  are H or CH₃;

[1146] or

[1147] R(3) and R(4)

[1148] independently of one another are (C₁-C₉)-heteroaryl,

[1149] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[1150] or

[1151] R(3) and R(4)

[1152] independently of one another are

[1153] Y is oxygen, —S— or —NR(22)—;

[1154] h, ad, ah independently are zero or 1;

[1155] i, j, k, ae, af, ag, ao, ap and ak independently are zero, 1, 2,3, 4,

[1156] but where in each case

[1157] h, i and k are not simultaneously zero,

[1158] ad, ae and ag are not simultaneously zero,

[1159] ah, ao and ak are not simultaneously zero,

[1160] R(23), R(24), R(25) and R(22)

[1161] independently are hydrogen or (C₁-C₃)-alkyl;

[1162] or

[1163] R(3) and R(4)

[1164] independently of one another are hydrogen, F, Cl, Br, I, CN,(C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(g)H_(2g)R(26);

[1165] g is zero, 1, 2, 3 or 4;

[1166] R(26) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1167] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group, consisting of F, Cl, CF₃, methyl,methoxy and

[1168] NR(27)R(28);

[1169] R(27) and R(28)

[1170] are H, (C₁-C₄)-alkyl or (C₁-C₄)-pefluoroalkyl;

[1171] or

[1172] R(3) and R(4)

[1173] independently of one another are SR(29), —OR(30), —NR(31)R(32) or—CR(33)R(34)R(35);

[1174] R(29), R(30), R(31) and R(33)

[1175] independently are —C_(a)H_(2a)—(C₁-C₉)-heteroaryl,

[1176] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[1177] a is zero, 1 or 2;

[1178] R(32), R(34) and R(35)

[1179] independently of one another are defined as R(29) or arehydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1180] or

[1181] R(3) and R(4)

[1182] independently of one another are

[1183] R(96), R(97) and R(98)

[1184] independently are (C₁-C₉)-heteroaryl,

[1185]  which is linked via C or N and which is unsubstituted orsubstituted by 1 to 3 substituents selected from the group consisting ofF, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino, dimethylamino orbenzyl;

[1186] W is oxygen, S or NR(36)—;

[1187] R(36) is H or (C₁-C₄)-alkyl;

[1188] or

[1189] R(3) and R(4)

[1190] independently of one another are R(37)—SO_(cm) orR(38)R(39)N—SO₂—;

[1191] cm is 1 or 2;

[1192] R(37) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenylor

[1193] —C_(s)H_(2s)R(40);

[1194] s is zero, 1, 2, 3 or 4;

[1195] R(40) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1196] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(41)R(42);

[1197] R(41) and R(42)

[1198]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1199] R(38) is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(w)H_(2w)—R(43);

[1200] w is zero, 1, 2, 3 or 4;

[1201] R(43) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1202] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(44)R(45);

[1203]  R(44) and R(45)

[1204]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1205] R(39) is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1206] or

[1207] R(38) and R(39)

[1208] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[1209] or

[1210] R(3) and R(4)

[1211] independently of one another are R(46)X(1)—;

[1212] X(1) is oxygen, S, NR(47), (D═O)A—, NR(48)C═MN^((*))R(49)—,

[1213] M is oxygen or S;

[1214] A is oxygen or NR(50);

[1215] D is C or SO;

[1216] R(46) is (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, (CH₂)_(b)C_(d)F_(2d+1)or —C_(x)H_(2x)—R(51);

[1217] b is zero or 1;

[1218] d is 1, 2, 3, 4, 5, 6 or 7;

[1219] x is zero, 1, 2, 3 or 4;

[1220] R(51) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1221] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(52)R(53);

[1222] R(52) and R(53)

[1223]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1224] R(47), R(48) and R(50)

[1225] independently are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-pefluoroalkyl;

[1226] R(49) is defined as R(46);

[1227] or

[1228] R(46) and R(47), or R(46) and R(48)

[1229] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl,

[1230] where A and N^((*)) are bonded to the phenyl nucleus of thebenzoylguanidine parent structure;

[1231] or

[1232] R(3) and R(4)

[1233] independently of one another are —SR(64), —OR(65), —NHR(66),—NR(67)R(68), —CHR(69)R(70), —C(OH)R(54)R(55), —C≡CR(56),—CR(58)═CHR(57), —[CR(59)R(60)]_(u)—(CO)—[CR(61)R(62)]_(v)—R(63);

[1234] R(64), R(65), R(66), R(67) and R(69)

[1235] identically or differently are—(CH₂)_(y)—(CHOH)_(z)—(CH₂)_(aa)—(CHOH)_(t)—R(71) or—(CH₂)_(ab)—O—(CH₂—CH₂O)_(ac)—R(72),

[1236] R(71) and R(72)

[1237] are hydrogen or methyl;

[1238] u is 1, 2, 3 or 4;

[1239] v is zero, 1, 2, 3 or 4;

[1240] y, z, aa, ab and ac

[1241] identically or differently are zero, 1, 2, 3 or 4;

[1242] t is 1, 2, 3 or 4;

[1243] R(68), R(70), R(54) and R(55)

[1244] identically or differently are hydrogen, (C₁-C₆)-alkyl;

[1245] or

[1246] R(69) and R(70), or R(54) and R(55)

[1247] together with the carbon atom carrying them are a(C3-C8)-cycloalkyl;

[1248] R(63)

[1249] is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or —C_(e)H_(2e)—R(73);

[1250] e is zero, 1, 2, 3 or 4;

[1251] R(56), R(57) and R(73)

[1252] independently are phenyl,

[1253] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(74)R(75);

[1254] R(74) and R(75)

[1255]  are H or (C₁-C₄)-alkyl;

[1256] or

[1257] R(56), R(57) and R(73)

[1258] independently are (C₁-C₉)-heteroaryl,

[1259] which is unsubstituted or substitued as phenyl;

[1260] R(58), R(59), R(60), R(61) and R(62)

[1261] are hydrogen or methyl,

[1262] or

[1263] R(3) and R(4)

[1264] independently of one another are R(76)—NH—SO₂—;

[1265] R(76) is R(77)R(78)N—(C═Y′)—;

[1266] Y′ is oxygen, S or N—R(79);

[1267] R(77) and R(78)

[1268] identically or differently are H, (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl,—C_(f)H_(2f)R(80);

[1269] f is zero, 1, 2, 3 or 4;

[1270] R(80) is (C₅-C₇)-cycloalkyl or phenyl,

[1271] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methoxy and(C₁-C₄)-alkyl;

[1272] or

[1273] R(77) and R(78)

[1274] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl,

[1275] R(79)

[1276] is defined as R(77) or is amidine;

[1277] or

[1278] R(3) and R(4)

[1279] independently of one another are NR(84)R(85);

[1280] R(84) and R(85)

[1281] independently of one another are H, (C₁-C₄)-alkyl, or togetherare 4 or 5 methylene groups,

[1282] of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃ orN-benzyl;

[1283] and their pharmaceutically tolerable salts;

[1284] (HOE 94/F 123—EP-A 682 017, NZ 272 058)

[1285] y) bicyclic heteroaroylguanidines of the formula I

[1286] in which:

[1287] T, U, V, W, X, Y and Z

[1288] independently of one another are nitrogen or carbon;

[1289] but with the restriction that X and Z are not simultaneouslynitrogen,

[1290] and that T, U, V, W, X, Y and Z carry no substituents if they arenitrogen,

[1291] and that no more than four of them are simultaneously nitrogen,

[1292] R(1) and R(2)

[1293] independently of one another are hydrogen, F, Cl, Br, I,(C₁-C₃)-alkyl, (C₁-C₃)-perfluoroalkyl, OR(8), NR(8)R(9) orC(═O)N═C(NH₂)₂;

[1294] R(8) and R(9)

[1295] independently of one another are hydrogen or (C₁-C₃)-alkyl,

[1296] or

[1297] R(8) and R(9)

[1298] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[1299] R(3), R(4), R(5), R(6) and R(7)

[1300] independently of one another are hydrogen, F, Cl, Br, I, —C≡N,

[1301] X_(k)—(CH₂)_(p)—(C_(q)F_(2q+1)), R(10a)—SO_(bm),R(10b)R(10c)N—CO, R(11)—CO— or

[1302] R(12)R(13)N—SO₂—,

[1303] where the perfluoroalkyl group is straight-chain or branched;

[1304] X is oxygen, S or NR(14);

[1305] R(14) is H or (C₁-C₃)-alkyl;

[1306] bm is zero, 1 or 2;

[1307] p is zero, 1 or 2;

[1308] k is zero or 1;

[1309] q 1, 2, 3, 4, 5 or 6;

[1310] R(10a), R(10b), R(11) and R(12)

[1311] independently of one another are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl,—C_(n)H_(2n)—R(15) or (C₁-C₈)-perfluoroalkyl;

[1312] n is zero, 1, 2, 3 or 4;

[1313] R(15) is (C₃-C₇)-cycloalkyl or phenyl, which is not substituted

[1314] or is substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and

[1315] NR(16)R(17);

[1316] R(16) and R(17)

[1317]  are H or C₁-C₄-alkyl;

[1318] or

[1319] R(10b), R(11) and R(12)

[1320] are hydrogen;

[1321] R(10c) and R(13)

[1322] independently are hydrogen or (C₁-C₄)-alkyl;

[1323] or

[1324] R(10b) and R(10c) and R(12) and R(13)

[1325] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[1326] or

[1327] R(3), R(4), R(5), R(6) and R(7)

[1328] independently of one another are (C₁-C₈)-alkyl,—C_(al)H_(2al)R(18) or (C₃-C₈)-alkenyl;

[1329] al is zero, 1 or 2;

[1330] R(18) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,where the

[1331] aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(19a)R(19b);

[1332] R(19a) and R(19b)

[1333] are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1334] or

[1335] R(3), R(4), R(5), R(6) and R(7)

[1336] independently of one another are (C₁-C₉)-heteroaryl, which islinked via C or N and which is unsubstituted or substituted by 1-3substituents from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino or dimethylamino;

[1337] or

[1338] R(3), R(4), R(5), R(6) and R(7)

[1339] independently of one another are

[1340] Y is oxygen, —S— or —NR(22)—;

[1341] h, ad, ah

[1342] independently of one another are zero or 1;

[1343] i, j, k, ae, af, ag, ao, ap and ak

[1344] independently of one another are zero, 1, 2, 3 or 4;

[1345] but where in each case

[1346] h, i and k are not simultaneously zero,

[1347] ad, ae and ag are not simultaneously zero, and

[1348] ah, ao and ak are not simultaneously zero,

[1349] R(23), R(24), R(25) and R(22)

[1350] independently of one another are hydrogen or (C₁-C₃)-alkyl;

[1351] or

[1352] R(3), R(4), R(5), R(6) and R(7)

[1353] independently of one another are SR(29), —OR(30), —NR(31)R(32) or

[1354] —CR(33)R(34)R(35);

[1355] R(29), R(30), R(31) and R(33)

[1356] independently of one another are —C_(a)H_(2a)—(C₁-C₉)-heteroaryl,which is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino;

[1357] a is zero, 1 or 2;

[1358] R(32), R(34) and R(35)

[1359] independently of one another are defined as R(29) or arehydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1360] or

[1361] R(3), R(4), R(5), R(6) and R(7)

[1362] independently of one another are

[1363] R(96), R(97) and R(98)

[1364] independently of one another are (C₁-C₉)-heteroaryl, which islinked via C or N and which is unsubstitued or substituted by 1 to 3substituents from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino, dimethylamino or benzyl;

[1365] W is oxygen, S or NR(36)—;

[1366] R(36) is H or (C₁-C₄)-alkyl;

[1367] or

[1368] R(3), R(4), R(5), R(6) and R(7)

[1369] independently of one another are R(46)X(1)—;

[1370] X(1) is oxygen, S, NR(47), (D═O)A— or NR(48)C═MN^((*))R(49)—;

[1371] M is oxygen or sulfur;

[1372] A is oxygen or NR(50);

[1373] D is C or SO;

[1374] R(46) is (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, (CH₂)_(b)C_(d)F_(2d+1)or —C_(x)H_(2x)—R(51);

[1375] b is zero or 1;

[1376] d is 1, 2, 3, 4, 5, 6 or 7;

[1377] x is zero, 1, 2, 3 or 4;

[1378] R(51) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1379] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(52)R(53);

[1380] R(52) and R(53)

[1381]  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1382] R(47), R(48) and R(50) independently

[1383] are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1384] R(49) is defined as R(46);

[1385] or

[1386] R(46) and R(47), or R(46) and R(48)

[1387] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[1388] where A and N^((*)) are bonded to the phenyl nucleus of theheteroaroylguanidine parent structure;

[1389] or

[1390] R(3), R(4), R(5), R(6) and R(7)

[1391] independently of one another are -SR(64), —OR(65), —NHR(66),—NR(67)R(68), —CHR(69)R(70) or —CR(54)R(55)OH, —C≡CR(56), —CR(58)═CR(57)or —[CR(59)R(60)]_(u)—CO—[CR(61)R(62)]_(v)—R(63);

[1392] R(64), R(65), R(66), R(67) and R(69)

[1393] identically or differently are

[1394] —(CH₂)_(y)—(CHOH)_(z)—(CH₂)_(aa)—(CHOH)_(t)—R(71) or

[1395] —(CH₂)_(ab)—O—(CH₂—CH₂O)_(ac)—R(72);

[1396] R(71) and R(72)

[1397] independently of one another are hydrogen or methyl;

[1398] u is 1, 2, 3 or 4;

[1399] v is zero, 1, 2, 3 or 4;

[1400] y, z, aa, ab and ac identically or differently

[1401] are zero, 1, 2, 3 or 4;

[1402] t is 1, 2, 3 or 4;

[1403] R(68), R(70), R(54) and R(55)

[1404] identically or differently are hydrogen or (C₁-C₆)-alkyl;

[1405] or

[1406] R(69) and R(70), or R(54) and R(55)

[1407] together with the carbon atom carrying them are(C3-C8)-cycloalkyl;

[1408] R(63)

[1409] is hydrogen, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(e)H_(2e)—R(73);

[1410] e is zero, 1, 2, 3 or 4;

[1411] R(56), R(57) and R(73) independently

[1412] are phenyl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(74)R(75);

[1413] R(74) and R(75)

[1414] are hydrogen or (C₁-C₄)-alkyl;

[1415] or

[1416] R(56), R(57) and R(73) independently

[1417] are (C₁-C₉)-heteroaryl, which is unsubstituted or substituted asphenyl;

[1418] R(58), R(59), R(60), R(61) and R(62)

[1419] are hydrogen or methyl;

[1420] or

[1421] R(3), R(4), R(5), R(6) and R(7)

[1422] independently of one another are R(76)—NH—SO₂—;

[1423] R(76) is R(77)R(78)N—(C═Y′)—;

[1424] Y′ is oxygen, S or N—R(79);

[1425] R(77) and R(78)

[1426] identically or differently are hydrogen, (C₁-C₈)-alkyl,(C₃-C₆)-alkenyl or —C_(f)H_(2f)—R(80);

[1427] f is zero, 1, 2, 3 or 4;

[1428] R(80) is (C₅-C₇)-cycloalkyl or phenyl, which is

[1429]  unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methoxy and (C₁-C₄)-alkyl;

[1430] or

[1431] R(77) and R(78)

[1432] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[1433] R(79) is defined as R(77) or is amidine;

[1434] or

[1435] R(3), R(4), R(5), R(6) and R(7)

[1436] independently of one another are NR(84a)R(85), OR(84b), SR(84c)or —C_(n)H_(2n)—R(84d);

[1437] n is zero, 1, 2, 3 or 4;

[1438] R(84d) is (C₃-C₇)-cycloalkyl or phenyl, which is not substituted

[1439] or is substituted by 1-3 substituents from the group consistingof F, Cl, CF₃, methyl, methoxy and NR(16)R(17);

[1440] R(16) and R(17)

[1441] are hydrogen, or C₁-C₄-alkyl;

[1442] R(84a), R(84b), R(84c) and R(85)

[1443] independently of one another are hydrogen, (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl or (CH₂)_(ax)—R(84g);

[1444] ax is zero, 1, 2, 3 or 4;

[1445] R(84g) is (C₃-C₇)-cycloalkyl or phenyl, which is not

[1446] substituted or is substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(84u)R(84v);

[1447] R(84u) and R(84v)

[1448] are hydrogen or C₁-C₄-alkyl;

[1449] or

[1450] R(84a) and R(85)

[1451] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl,

[1452] and their pharmaceutically tolerable salts;

[1453] (HOE 94/F 134—EP-A 686 627, NZ 272 103)

[1454] z) benzoylguanidines of the formula I

[1455] in which:

[1456] R(1) is R(6)—SO_(m);

[1457] m is zero, 1 or 2;

[1458] R(6) is perfluoroalkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,which

[1459] is straight-chain or branched;

[1460] R(2) and R(3)

[1461] independently of one another are hydrogen, F, Cl, Br, I, alkylhaving 1, 2, 3 or 4 carbon atoms, alkoxy having 1, 2, 3 or 4 carbonatoms or phenoxy,

[1462] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, methyl and methoxy;methoxy;

[1463] or

[1464] R(2) and R(3)

[1465] independently of one another are pyrrol-1-yl, pyrrol-2-yl- orpyrrol-3-yl,

[1466] which is not substituted or is substituted by 1 to 4 substituentsselected from the group consisting of F, Cl, Br, I, CN, alkanoyl having2, 3, 4, 5, 6, 7 or 8 carbon atoms, alkoxycarbonyl having 2, 3, 4, 5, 6,7 or 8 carbon atoms, formyl, carboxyl, CF₃, methyl and methoxy;

[1467] R(4) and R(5)

[1468] independently of one another are hydrogen, alkyl having 1, 2 or 3carbon atoms, F, Cl, Br, I, CN, OR(7), NR(8)R(9) or

[1469] —(CH₂)_(n)—(CF₂)_(o)—CF₃;

[1470] R(7), R(8) and R(9)

[1471] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[1472] n is zero or 1;

[1473] o is zero, 1 or 2;

[1474] and their pharmacologically acceptable salts;

[1475] (HOE 94/F 168—EP-A 690 048, NZ 272 373)

[1476] ab) phenyl-substituted alkenylcarboxylic acid guanidides,carrying perfluoroalkyl groups, of the formula I

[1477] in which:

[1478] R(A) is hydrogen, F, Cl, Br, I, CN, OH, OR(6), (C₁-C₈)-alkyl,

[1479] O_(r)(CH₂)_(a)C_(b)F_(2b+1), (C₃-C₈)-cycloalkyl or NR(7)R(8);

[1480] r is zero or 1;

[1481] a is zero, 1, 2, 3 or 4;

[1482] b is 1, 2, 3, 4, 5, 6, 7 or 8;

[1483] R(6) is (C₁-C₈)-alkyl, (C₁-C₄)-perfluoroalkyl, (C₃-C₈)-alkenyl,(C₃-C₈)-cycloalkyl, phenyl or benzyl;

[1484] where the aromatics are not substituted or are substituted by 1-3substituents from the group consisting of F, Cl, CF₃, methyl, methoxyand

[1485] NR(9)R(10);

[1486] R(9) and R(10)

[1487] are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1488] R(7) and R(8)

[1489] independently of one another are defined as R(6);

[1490] or

[1491] R(7) and R(8)

[1492] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[1493] R(B) independently is defined as R(A);

[1494] X is zero, 1 or 2;

[1495] Y is zero, 1 or 2;

[1496] R(C) is hydrogen, F, Cl, Br, I, CN, OR(12), (C₁-C₈)-alkyl,O_(p)(CH₂)_(f)C_(g)F_(2g+1)

[1497] or (C₃-C₈)-cycloalkyl;

[1498] p is zero or 1;

[1499] f is zero, 1, 2, 3 or 4;

[1500] g is 1, 2, 3, 4, 5, 6, 7 or 8;

[1501] R(12)

[1502] is (C₁-C₈)-alkyl, (C₁-C₄)-perfluoroalkyl, (C₃-C₈)-alkenyl,(C₃-C₈)-cycloalkyl, phenyl or benzyl;

[1503] where the aromatics phenyl or benzyl are not substituted or aresubstituted by 1-3 substituents from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(13)R(14);

[1504] R(13) and R(14)

[1505]  independently of one another are H, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl;

[1506] R(D) independently is defined as R(C),

[1507] R(1) is hydrogen, (C₁-C₈)-alkyl, —O_(t)(CH₂)_(d)C_(e)F_(2e+1),(C₃-C₈)-cycloalkyl, F, Cl, Br, I or CN;

[1508] t is zero or 1;

[1509] d is zero, 1, 2, 3 or 4;

[1510] e is 1, 2, 3, 4, 5, 6, 7 or 8;

[1511] R(2), R(3), R(4) and R(5)

[1512] independently of one another are defined as R(1);

[1513] but with the condition that at least one of the substituentsR(A), R(B), R(C), R(D), R(1), R(2), R(4) or R(5) is anO_(r)(CH₂)_(a)C_(b)F_(2b+1), O_(p)(CH₂)_(f)C_(g)F_(2g+1) orO_(t)(CH₂)_(d)C_(e)F_(2e+1) group and R(3) is not anO_(t)(CH₂)_(d)C_(e)F_(2e+1) group;

[1514] and their pharmaceutically tolerable salts;

[1515] (HOE 94/F 182—EP-A 690 048, NZ 272 449)

[1516] ac) ortho-amino-substituted benzoylguanidines of the formula I

[1517] in which:

[1518] R(1) is NR(50)R(6),

[1519] R(50) and R(6)

[1520] independently of one another are hydrogen, (C₁-C₈)-alkyl or(C₁-C₈)-perfluoroalkyl;

[1521] R(2), R(3), R(4) and R(5)

[1522] independently of one another are R(10)—SO_(a)—, R(11)R(12)N—CO—,R(13)—CO— or R(14)R(15)N—SO₂—;

[1523] a is zero, 1 or 2,

[1524] R(10), R(11), R(12), R(13), R(14) and R(15)

[1525] independently of one another are (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl, (C₃-C₆)-alkenyl or —C_(ab)H_(2ab)—R(16);

[1526] ab is zero, 1, 2, 3 or 4;

[1527] R(16) is (C₃-C₇)-cycloalkyl, phenyl,

[1528] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy orNR(,17)R(18);

[1529] R(17) and R(18)

[1530]  independently of one another are H, CF₃ or (C₁-C₄)-alkyl;

[1531] or

[1532] R(11), R(12), and also R(14) and R(15)

[1533] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[1534] or

[1535] R(11), R(12), R(14) and R(15)

[1536] independently of one another are hydrogen;

[1537] or

[1538] R(2), R(3), R(4) and R(5)

[1539] independently of one another are SR(21), —OR(22), —NR(23)R(24) or—CR(25)R(26)R(27);

[1540] R(21), R(22), R(23) and R(25)

[1541] independently of one another are —C_(b)H_(2b)—(C₁-C₉)-heteroaryl,which is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino;

[1542] b is zero, 1 or 2;

[1543] R(24), R(26) and R(27)

[1544] independently of one another are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl;

[1545] or

[1546] R(2), R(3), R(4) and R(5)

[1547] independently of one another are hydrogen, F, Cl, Br, I, CN,

[1548] —(Xa)_(dg)—C_(da)H_(2da+1),—(Xb)_(dh)—(CH₂)_(db)—C_(de)F_(2de+1), (C₃-C₈)-alkenyl or

[1549] —C_(df)H_(2df)R(30);

[1550] (Xa) is O, S or NR(33);

[1551] R(33)

[1552] is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1553] dg is zero or 1;

[1554] (Xb) is O, S or NR(34);

[1555] R(34)

[1556] is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1557] dh is zero or 1;

[1558] da is zero, 1, 2, 3, 4, 5, 6, 7, 8;

[1559] db is zero, 1, 2, 3, 4;

[1560] de is zero, 1, 2, 3, 4, 5, 6, 7;

[1561] df is zero, 1, 2, 3, 4;

[1562] R(30)

[1563] is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where thearomatics phenyl, biphenylyl or naphthyl are not substituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and

[1564] NR(31)R(32);

[1565] R(31) and R(32)

[1566] are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1567] or

[1568] R(2), R(3), R(4) and R(5)

[1569] independently of one another are NR(40)R(41) or

[1570] —(Xe)—(CH₂)_(eb)R(45);

[1571] R(40) and R(41)

[1572] independently of one another are hydrogen, (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl or (CH₂)_(e)—R(42);

[1573] e is zero, 1, 2, 3 or 4;

[1574] R(42)

[1575] is (C₃-C₇)-cycloalkyl, phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and

[1576] NR(43)R(44);

[1577] R(43) and R(44)

[1578]  independently of one another are H, CF₃ or (C₁-C₄)-alkyl;

[1579] or

[1580] R(40) and R(41)

[1581] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[1582] (Xe) is O, S or NR(47);

[1583] R(47)

[1584]  is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1585] eb is zero, 1, 2, 3 or 4;

[1586] R(45) is (C₃-C₇)-cycloalkyl, phenyl, which is not substituted oris

[1587] substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy, NR(50)R(51) and

[1588] —(Xfa)—(CH₂)_(ed)—(Xfb)R(46);

[1589] Xfa is CH₂, O, S or NR(48);

[1590] Xfb is O, S or NR(49);

[1591] ed is 1, 2, 3 or 4;

[1592] R(46)

[1593] is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1594] R(48), R(49), R(50) and R(51)

[1595] independently of one another are H or (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl;

[1596] where R(3) and R(4), however, cannot be hydrogen,

[1597] and their pharmaceutically tolerable salts;

[1598] (HOE 94/F 265—NZ 272 946, EP-A 700 904)

[1599] ad) benzoylguanidines of the formula I

[1600] in which:

[1601] one of the three substituents R(1), R(2) and R(3)

[1602] is (C₁-C₉)-heteroaryl-N—oxide,

[1603] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[1604] or

[1605] one of the three substituents R(1), R(2) and R(3)

[1606] is —SR(10), —OR(10), —NR(10)R(11) or —CR(10)R(11)R(12);

[1607] R(10)

[1608] is —C_(a)H_(2a)—(C₁-C₉)-heteroaryl-N-oxide,

[1609] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[1610] a is zero, 1 or 2;

[1611] R(11) and R(12)

[1612] independently of one another are defined as R(10), are hydrogenor (C₁-C₄)-alkyl;

[1613] and the other substituents R(1), R(2) and R(3) in each case

[1614] independently of one another are (C₁-C₈)-alkyl, (C₂-C₈)-alkenylor

[1615] —C_(m)H_(2m)R(14);

[1616] m is zero, 1 or 2;

[1617] R(14) is (C₃-C₈)-cycloalkyl or phenyl,

[1618] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃₁ methyl, methoxy and

[1619] NR(15)R(16),

[1620] R(15) and R(16)

[1621]  are hydrogen or CH₃;

[1622] or

[1623] the other substituents R(1), R(2) and R(3) in each case

[1624] independently of one another are hydrogenq, F, Cl, Br, I, —C≡N,

[1625] X—(CH₂)_(p)—(C_(q)F_(2q+1)), R(22)—SO_(u), R(23)R(24)N—CO,R(25)—CO— or

[1626] R(26)R(27)N—SO₂—,

[1627] where the perfluoroalkyl group is straight-chain or branched;

[1628] X is a bond, oxygen, S or NR(28);

[1629] u is zero, 1 or 2;

[1630] is zero, 1 or 2;

[1631] is zero, 1, 2, 3, 4, 5 or 6;

[1632] R(22), R(23), R(25) and R(26)

[1633] independently are (C₁-C₈)-alkyl, (C₂-C₆)-alkenyl,—C_(n)H_(2n)—R(29)

[1634] or CF₃;

[1635] n is zero, 1, 2, 3 or 4;

[1636] R(28) is hydrogen or (C₁-C₃)-alkyl;

[1637] R(29) is (C₃-C7)-cycloalkyl or phenyl;

[1638] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy and

[1639] NR(30)R(31);

[1640] R(30) and R(31)

[1641]  are hydrogen or C₁-C₄-alkyl,

[1642] or

[1643] R(23), R(25) and R(26)

[1644] are also hydrogen;

[1645] R(24) and R(27)

[1646] independently of one another are hydrogen or (C₁-C₄)-alkyl;

[1647] or

[1648] R(23) and R(24), and also R(26) and R(27) together are 4 or 5methylene groups, of which one CH₂ group can be replaced by oxygen, S,NH, N—CH₃ or N-benzyl;

[1649] or

[1650] the other substituents R(1), R(2) and R(3) in each case

[1651] independently of one another are OR(35) or NR(35)R(36);

[1652] R(35) and R(36)

[1653] independently of one another are hydrogen or (C₁-C₆)-alkyl;

[1654] or

[1655] R(35) and R(36)

[1656] together are 4-7 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl,

[1657] R(4) and R(5)

[1658] independently of one another are hydrogen, (C₁-C₄)-alkyl, F, Cl,

[1659] —OR(32), —NR(33)R(34) or C_(r)F_(2r+1);

[1660] R(32), R(33) and R(34)

[1661] independently of one another are hydrogen or (C₁-C₃)-alkyl;

[1662] r is 1, 2, 3 or 4;

[1663] and their pharmaceutically tolerable salts;

[1664] (HOE 94/F 266—EP-A 702 001, NZ 272 948)

[1665] ae) benzoylguanidines of the formula I

[1666] in which:

[1667] R(1) is hydrogen, F, Cl, Br, I, CN, NO₂, OH, (C₁-C₈)-alkyl,(C₃-C₈)-cycloalkyl, O_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃;

[1668] a is zero or 1;

[1669] b is zero, 1 or 2;

[1670] c is zero, 1, 2 or 3;

[1671] or

[1672] R(1) is R(5)—SO_(m) or R(6)R(7)N—SO₂—;

[1673] m is zero, 1 or 2;

[1674] R(5) and R(6) independently of one another

[1675] are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, CF₃ or —C_(n)H_(2n)—R(8);

[1676] n is zero, 1, 2, 3 or 4;

[1677] R(7) is hydrogen or (C₁-C₄)-alkyl;

[1678] R(8) is (C₃-C₇)-cycloalkyl or phenyl,

[1679] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10);

[1680] R(9) and R(10) independently of one another

[1681] are hydrogen or (C₁-C₄)-alkyl;

[1682] or

[1683] R(6) is H;

[1684] or R(6) and R(7)

[1685] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl,

[1686] or

[1687] R(1) is —SR(11), —OR(11) or —CR(11)R(12)R(13);

[1688] R(11) is —C_(p)H_(2p)—(C₃-C₈)-cycloalkyl, —(C₁-C₉)-heteroaryl orphenyl,

[1689] where the aromatic systems are unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino;

[1690] R(12), R(13) independently of one another

[1691] are defined as R(11) or are hydrogen or (C₁-C₄)-alkyl;

[1692] p is zero, 1 or 2;

[1693] or

[1694] R(1) is phenyl, naphthyl, biphenylyl or (C₁-C₉)-heteroaryl, thelatter linked via C or N,

[1695] which are unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[1696] R(2) is —CF₂R(14), —CF[R(15)][R(16)], —CF[(CF₂)_(q)—CF₃)][R(15)],—C[(CF₂)_(r)—CF₃]═CR(15)R(16);

[1697] R(14) is (C₁-C₄)-alkyl or (C₃-C₆)-cycloalkyl;

[1698] R(15) and R(16) independently of one another

[1699] are hydrogen or (C₁-C₄)-alkyl;

[1700] q is zero, 1 or 2;

[1701] r is zero, 1 or 2;

[1702] R(3) is defined as R(1);

[1703] R(4) is hydrogen, (C₁-C₃)-alkyl, F, Cl, Br, I, CN,—(CH₂)_(s)—(CF₂)_(t)—CF₃;

[1704] s is zero or 1;

[1705] t is zero, 1 or 2;

[1706] and their pharmaceutically tolerable salts;

[1707] (HOE 94/F 267—EP-A 700 899, NZ 272 947)

[1708] af) benzoylguanidines of the formula I

[1709] in which:

[1710] one of the three substituents R(1), R(2) and R(3)

[1711] is —Y-4—[(CH₂)_(k)—CHR(7)—(C═O)R(8)]-phenyl,

[1712] —Y-3—(CH₂)_(k)—CHR(7)—(C═O)R(8)]-phenyl or

[1713] —Y-2—[(CH₂)_(k)—CHR(7)—(C═O)R(8)]-phenyl,

[1714] where the phenyl in each case is unsubstituted or substituted by1-2 substituents from the group F, Cl, —CF₃, methyl, hydroxyl, methoxy,or —NR(37)R(38);

[1715] R(37) and R(38)

[1716] independently of one another are hydrogen or —CH3;

[1717] Y is a bond, oxygen, —S— or —NR(9);

[1718] R(9) is hydrogen or —(C₁-C₄)-alkyl;

[1719] R(7) is —OR(10) or —NR(10)R(11);

[1720] R(10) and R(11)

[1721]  independently of one another are hydrogen, —(C₁-C₈)-alkyl,—(C₁-C₈)-alkanoyl, —(C₁-C₈)-alkoxycarbonyl, benzyl, benzyloxycarbonyl;

[1722] or

[1723] R(10) is trityl;

[1724] R(8) is —OR(12) or —NR(12)R(13);

[1725] R(12) and R(13)

[1726]  independently of one another are hydrogen, —(C₁-C₈)-alkyl orbenzyl;

[1727] k is zero, 1, 2, 3 or 4;

[1728] and the other radicals R(1), R(2) and R(3) in each case

[1729] independently of one another are —(C₁-C₈)-alkyl, —(C₂-C₈)-alkenylor

[1730] —(CH₂)_(m)R(14);

[1731] m is zero, 1 or 2;

[1732] R(14) is —(C₃-C₈)-cycloalkyl or phenyl,

[1733] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, —CF₃, methyl, methoxy and—N R(15)R(16);

[1734] R(15) and R(16)

[1735] are hydrogen or —CH₃;

[1736] or

[1737] the other radicals R(1), R(2) and R(3) in each case

[1738] independently of one another are R(18)R(19)N—(C═Y′)—NH—SO₂—;

[1739] Y′ is oxygen, —S— or —N—R(20);

[1740] R(18) and R(19)

[1741] independently of one another are hydrogen, —(C₁-C₈)-alkyl,—(C₃-C₆)-alkenyl or —(CH₂)_(t)—R(21);

[1742] t is zero, 1, 2, 3 or 4;

[1743] R(21) is —(C₅-C₇)-cycloalkyl or phenyl,

[1744] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, —CF₃, methoxy and—(C₁-C₄)-alkyl;

[1745] or

[1746] R(18) and R(19)

[1747] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, —S—, —NH—, —N—CH₃ or —N-benzyl;

[1748] R(20)

[1749] is defined as R(18) or is amidine;

[1750] or

[1751] the other radicals R(1), R(2) and R(3) in each case

[1752] independently of one another are hydrogen, F, Cl, Br, I, —C≡N,X—(CH₂)_(p)—(C_(q)F_(2q+1)), R(22)—SO_(u)—, R(23)R(24)N—CO—, R(25)—CO—or R(26)R(27)N—SO₂—, where the perfluoroalkyl group is straight-chain orbranched;

[1753] X is a bond, oxygen, —S— or —NR(28);

[1754] u is zero, 1 or 2;

[1755] is zero, 1 or 2;

[1756] q is 1, 2, 3, 4, 5 or 6;

[1757] R(22), R(23), R(25) and R(26)

[1758] independently of one another are —(C₁-C₈)-alkyl,—(C₃-C₆)-alkenyl, —(CH₂)_(n)—R(29) or —CF₃;

[1759] n is zero, 1, 2, 3 or 4;

[1760] R(28) is hydrogen or —(C₁-C₃)-alkyl;

[1761] R(29) is —(C₃-C₇)-cycloalkyl or phenyl,

[1762] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, —CF₃, methyl, methoxy and—NR(30)R(31);

[1763] R(30) and R(31)

[1764]  are hydrogen or —(C₁-C₄)-alkyl;

[1765] or

[1766] R(23), R(25) and R(26)

[1767] are hydrogen;

[1768] R(24) and R(27)

[1769] independently of one another are hydrogen or —(C₁-C₄)-alkyl;

[1770] or

[1771] R(23) and R(24), and also R(26) and R(27)

[1772] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, —S—, —NH—, —N—CH₃ or —N-benzyl;

[1773] or

[1774] the other radicals R(1), R(2) and R(3) in each case

[1775] independently of one another are —OR(35) or —NR(35)R(36);

[1776] R(35) and R(36)

[1777] independently of one another are hydrogen or —(C₁-C₆)-alkyl;

[1778] or

[1779] R(35) and R(36)

[1780] together are 4-7 methylene groups, of which one CH₂ group

[1781] can be replaced by oxygen, —S—, —NH—, —N—CH₃ or —N-benzyl;

[1782] R(4) and R(5)

[1783] independently of one another are hydrogen, —(C₁-C₄)-alkyl, F, Cl,—OR(32), —NR(33)R(34) or —C_(r)F_(2r+1);

[1784] R(32), R(33) and R(34)

[1785] independently of one another are hydrogen or —(C₁-C₃)-alkyl;

[1786] r is 1, 2, 3 or 4;

[1787] and their pharmaceutically tolerable salts;

[1788] (HOE 94/F 352—EP-A 713 684, NZ 280 517)

[1789] ag) benzoylguanidines of the formula I

[1790] in which:

[1791] R(1) is R(6)—CO or R(7)R(8)N—CO;

[1792] R(6) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl

[1793] or —C_(n)H_(2n)—R(9),

[1794] n is zero, 1, 2, 3 or 4;

[1795] R(9) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1796] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and

[1797] NR(10)R(11),

[1798] R(10) and R(11)

[1799]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1800] R(7) is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenylor —C_(n)H_(2n)—R(12);

[1801] n is zero, 1, 2, 3 or 4;

[1802] R(12) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1803] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(13)R(14);

[1804] R(13) and R(14)

[1805]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1806] R(8) is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1807] or

[1808] R(7) and R(8) together

[1809] are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[1810] R(2) is defined as R(1), or is H, OH, F, Cl, Br, I, CN, NO₂,(C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(n)H_(2n)R(15);

[1811] n is zero, 1, 2, 3 or 4;

[1812] R(15) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1813] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(16)R(17);

[1814] R(16) and R(17)

[1815] are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1816] or

[1817] R(2) is (C₁-C₉)-heteroaryl,

[1818] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[1819] or

[1820] R(2) is SR(18), —OR(18), —NR(18)R(19) or —CR(18)R(19)R(20);

[1821] R(18) is —C_(a)H_(2a)—(C₁-C₉)-heteroaryl,

[1822] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino, dimethylamino;

[1823] a is zero, 1 or 2;

[1824] R(19) and R(20)

[1825] independently of one another are defined as R(18) or arehydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1826] or

[1827] R(2) is R(21)—SO_(m) or R(22)R(23)N—SO₂—;

[1828] m is 1 or 2;

[1829] R(21) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenylor —C_(n)H_(2n)—R(24);

[1830] n is zero, 1, 2, 3 or 4;

[1831] R(24) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1832] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(27)R(28);

[1833] R(27) and R(28)

[1834]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1835] R(22) is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(n)H_(2n)—R(29);

[1836] n is zero, 1, 2, 3 or 4;

[1837] R(29) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1838] where the aromatics are not substituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(30)R(31);

[1839] R(30) and R(31)

[1840]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1841] R(23) is hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1842] or

[1843] R(22) and R(23)

[1844] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃or N-benzyl;

[1845] or

[1846] R(2) is R(33)X—;

[1847] X is oxygen, S, NR(34), (D═O)A— or NR(34)C═MN^((*))R(35)—;

[1848] M is oxygen or S;

[1849] A is oxygen or NR(34);

[1850] D is C or SO;

[1851] R(33) is (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, (CH₂)_(b)C_(d)F_(2d+1)or —C_(n)H_(2n)—R(36);

[1852] b is zero or 1;

[1853] d is 1, 2, 3, 4, 5, 6 or 7;

[1854] n is zero, 1, 2, 3, or 4;

[1855] R(36) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,

[1856]  where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(37)R(38);

[1857]  R(37) and R(38)

[1858]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1859] R(34) is hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[1860] R(35) is defined as R(33);

[1861] or

[1862] R(33) and R(34)

[1863]  together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[1864]  where A and N^((*)) are bonded to the phenyl nucleus of thebenzoylguanidine parent structure;

[1865] or

[1866] R(2) is —SR(40), —OR(40), —NHR(40), —NR(40)R(41), —CHR(40)R(42),—CR(42)R(43)OH, —C≡CR(45), —CR(46)═CR(45) or—[CR(47)R(48)]_(u)—CO—[C(R49)R(50)]_(v)—R(44);

[1867] R(40) and R(41)

[1868] independently of one another are—(CH₂)_(p)—(CHOH)_(q)—(CH₂)_(r)—(CHOH)_(t)—R(51) or—(CH₂)_(p)—O—(CH₂—CH₂O)_(q)—R(51);

[1869] R(51) is hydrogen or methyl;

[1870] u is 1, 2, 3 or 4;

[1871] v is zero, 1, 2, 3 or 4;

[1872] p, q and r

[1873] independently of one another are zero, 1, 2, 3 or 4;

[1874] t is 1, 2, 3 or 4;

[1875] R(42) and R(43)

[1876] independently of one another are hydrogen or (C₁-C₆)-alkyl;

[1877] or

[1878] R(42) and R(43)

[1879] together with the carbon atom carrying them are a(C₃-C₈)-cycloalkyl;

[1880] R(44) is hydrogen, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl,—C_(e)H_(2e)—R(45);

[1881] e is zero, 1, 2, 3 or 4;

[1882] R(45) is phenyl,

[1883] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(52)R(53);

[1884] R(52) and R(53)

[1885] are H or (C₁-C₄)-alkyl;

[1886] or

[1887] R(45) is (C₁-C₉)-heteroaryl,

[1888] which is unsubstituted or substituted as phenyl;

[1889] or

[1890] R(45) is (C₁-C₆)-alkyl,

[1891] which is unsubstituted or substituted by 1-3 OH;

[1892] R(46), R(47), R(48), R(49) and R(50)

[1893] independently of one another are hydrogen or methyl;

[1894] or

[1895] R(2) is R(55)—NH—SO₂—;

[1896] R(55) is R(56)R(57)N—(C═Y)—;

[1897] Y is oxygen, S or N—R(58);

[1898] R(56) and R(57)

[1899] independently of one another are hydrogen, (C₁-C₈)-alkyl,(C₃-C₆)-alkenyl or —C_(f)H_(2f)—R(59);

[1900] f is zero, 1, 2, 3 or 4;

[1901] R(59) is (C₅-C₇)-cycloalkyl, phenyl,

[1902] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methoxy and(C₁-C₄)-alkyl;

[1903] or

[1904] R(56) and R(57)

[1905] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[1906] R(58)

[1907] is defined as R(56) or is amidine;

[1908] R(3), R(4) and R(5) are independently of one another defined asR(1) or R(2), but where at least one of the substituents R(2), R(3),R(4) and R(5) must be OH;

[1909] and their pharmaceutically tolerable salts;

[1910] (HOE 95/F 007 K—EP-A 723 956, NZ 280 887)

[1911] ah) benzoylguanidines of the formula I

[1912] in which:

[1913] one of the three substituents R(1), R(2) and R(3)

[1914] is R(6)—A—B—D—;

[1915] R(6) is a basic protonatable radical, i.e. an amino group—NR(7)R(8), an amidino group R(7)R(8)N—C[═N—R(9)]— or a guanidino group

[1916] R(7), R(8), R(9) and R(10)

[1917] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[1918] or

[1919] R(7) and R(8)

[1920] together are C_(a)H_(2a);

[1921] a is 4, 5, 6 or 7;

[1922] where if a =5, 6 or 7 a methylene group of the group C_(a)H_(2a)can be replaced by a heteroatom group O, SO_(m) or NR(11),

[1923] or

[1924] R(8) and R(9) or R(9) and R(10) or R(7) and R(10)

[1925] are a group C_(a)H_(2a);

[1926] a is 2, 3, 4 or 5;

[1927]  where if a=3, 4 or 5 a methylene group of the group C_(a)H_(2a)can be replaced by a heteroatom group O, SO_(m) or NR(11);

[1928] m is zero, 1 or 2;

[1929] R(11) is hydrogen or methyl;

[1930] or

[1931] R(6) is a basic heteroaromatic ring system having 1-9 carbonatoms;

[1932] A is C_(b)H_(2b);

[1933] b is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10;

[1934] where in the group C_(b)H_(2b) one or two methylene groups can bereplaced by one of the groupings selected from the group consisting of—O—, —CO—, —CH[OR(20)]—, —SO_(m)—, —NR(20)—, —NR(20)—CO—,—NR(20)—CO—NH—, —NR(20)—CO—NH—SO₂—,

[1935]  and —SO_(aa)[NR(19)]_(bb)—;

[1936] and where in the group C_(b)H_(2b) a methylene group can bereplaced by —CH—R(99), where R(99) together with R(7) forms apyrrolidine or piperidine ring;

[1937]  aa is 1 or 2;

[1938]  bb is 0 or 1;

[1939]  aa+bb=2;

[1940]  R(19) is hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[1941]  R(20) is hydrogen or methyl;

[1942] B is a phenylene or naphthylene radical

[1943] R(12) and R(13)

[1944] independently of one another are hydrogen, methyl, F, Cl, Br, ICF₃ or —SO_(w)—R(14);

[1945] R(14) is methyl or NR(15)R(16);

[1946] R(15) and R(16)

[1947]  independently of one another are hydrogen or alkyl having 1, 2,3 or 4 carbon atoms;

[1948] w is zero, 1 or 2;

[1949] D is —C_(d)H_(2d)—X_(f)—;

[1950] d is zero, 1, 2, 3 or 4;

[1951] X is —O—, —CO—, —CH[OR(21)]—, —SO_(m)— or —NR(21)—;

[1952] f is zero or 1;

[1953] R(21) is hydrogen or methyl;

[1954] m is zero, 1 or 2;

[1955] and the other substituents R(1) and R(2) and R(3) in each case

[1956] independently of one another are hydrogen, F, Cl, Br, I, —CN,—(C₁-C₈)-alkyl, —(C₂-C₈)-alkenyl, —NR(35)R(36) orR(17)—C_(g)H_(2g)—Z_(h)—;

[1957] g is zero, 1, 2, 3 or 4;

[1958] h is zero or 1;

[1959] R(35) and R(36)

[1960] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5 or 6 carbon atoms;

[1961] or

[1962] R(35) and R(36)

[1963] together are 4-7 methylene groups, of which one CH₂ group can bereplaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[1964] Z is —O—, —CO—, —SO_(v)—,—NR(18)—, —NR(18)—CO—, —NR(18)—CO—NH— or—NR(18)—SO₂—;

[1965] R(18) is hydrogen or methyl;

[1966] v is zero, 1 or 2;

[1967] R(17) is hydrogen, cycloalkyl having 3, 5 or 6 carbon atoms orC_(k)F_(2k+1)—;

[1968] k is 1, 2 or 3,

[1969] or

[1970] R(17) is pyrrol-1-yl, pyrrol-2-yl or pyrrol-3-yl,

[1971] which is not substituted or is substituted by 1-4 substituentsselected from the group consisting of F, Cl, Br, I, —CN,(C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃, methyland methoxy;

[1972] or

[1973] R(17) is (C₃-C₈)-cycloalkyl or phenyl,

[1974] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, hydroxyl,methoxy, —NR(37)R(38), CH₃SO₂— and H₂NO₂S—;

[1975] R(37) and R(38)

[1976] are hydrogen or —CH₃;

[1977] R(4) and R(5)

[1978] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, F, Cl, —OR(32), —NR(33)R(34) or —C_(r)F_(2r+1);

[1979] R(32), R(33) and R(34)

[1980] independently of one another are hydrogen or alkyl having 1, 2 or3 carbon atoms;

[1981] r is 1, 2, 3 or 4;

[1982] and their pharmacologically tolerable salts;

[1983] (HOE 95/F 072—EP-A 738 712, NZ 286 380)

[1984] ai) indenoylguanidines of the formula I

[1985] in which:

[1986] R(1) and R(2)

[1987] independently of one another are hydrogen, alkyl having 1, 2, 3,4, 5, 6, 7, 8, 9 or 10 carbon atoms, cycloalkyl having 3, 4, 5 or 6carbon atoms, O-alkyl having 1, 2, 3 or 4 carbon atoms, O—C(═O)-alkylhaving 1, 2, 3 or 4 carbon atoms or C_(m)H_(2m)—NR(12)R(13);

[1988] R(12) and R(13)

[1989] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[1990] m is zero, 1, 2, 3 or 4;

[1991] NH—C(═O)—NH₂, C(═O)—O-alkyl having 1, 2, 3 or 4 carbon atoms,C(═O)—NH₂, C(═O)—NH-alkyl having 1, 2, 3 or 4 carbon atoms,C(═O)—N(alkyl)₂ having 1, 2, 3 or 4 carbon atoms in each alkyl group,alkenyl having 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms, alkynyl having2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms, alkylaryl having 1, 2, 3 or 4carbon atoms in the alkyl group, alkenylaryl having 2, 3, 4, 5, 6, 7, 8,9 or 10 carbon atoms in the alkenyl group, alkynylaryl having 2, 3, 4,5, 6, 7, 8, 9 or 10 carbon atoms in the alkynyl group,C₁-C₄-alkyl-substituted aryl, C₁-C₄-alkylheteroaryl,C₁-C₄-alkenylheteroaryl, aminoalkylaryl having 1, 2, 3 or 4 carbon atomsin the alkyl group, substituted aryl, heteroaryl and substitutedheteroaryl;

[1992] R(3), R(4), R(5) and R(6)

[1993] independently of one another are hydrogen, alkyl having 1, 2, 3,4, 5, 6, 7, 8, 9 or 10 carbon atoms, O-alkyl having 1, 2, 3, 4, 5, 6, 7,8, 9 or 10 carbon atoms, halogen, (such as F, Cl, Br, I), OH, aryl,substituted aryl, heteroaryl, substituted heteroaryl, O-lower alkyl,O-aryl, O-lower alkylaryl, O-substituted aryl, O-lower alkyl-substitutedaryl, O—C(═O)—C₁-C₄-alkylaryl, O—C(═O)—N H—C₁-C₄-alkyl,O—C(═O)—N(C₁-C₄-alkyl)₂, NO₂, CN, CF₃, NH₂, NH—C(═O)—C₁-C₄-alkyl,NH—C(═O)—NH₂, COOH, C(═O)—O—C₁-C₄-alkyl, C(═O)—NH₂,C(—O)—NH—C₁-C₄-alkyl, C(═O)—N(C₁-C₄-alkyl)₂, C₁-C₄—COOH, C₁-C₄-alkyl-C(═O)—O—C₁-C₄-alkyl, SO₃H, SO₂-alkyl, SO₂-alkylaryl, SO₂—N-(alkyl)₂,SO₂—N(alkyl)(alkylaryl), C(═O)—R(11), C₁-C₁₀-alkyl-C(═O)—R(11),C₂-C₁₀-alkenyl-C(═O)—R(11), C₂-C₁₀-alkynyl-C(═O)—R(11),NH—C(═O)—C₁-C₁₀-alkyl-C(═O)—R(11), O—C₁-C₁₁-alkyl-C(═O)—R(11);

[1994] R(11) is C₁-C₄-alkyl, C₁-C₄-alkynyl, aryl, substituted aryl, NH₂,NH—C₁-C₄-alkyl, N—(C₁-C₄-alkyl)₂, SO₃H, SO₂-alkyl, SO₂-alkylaryl,SO₂—N-(alkyl)₂, SO₂—N(alkyl)(alkylaryl);

[1995] X is O, S or NH;

[1996] R(7), R(8), R(9) and R(10)

[1997] independently of one another are hydrogen, alkyl, cycloalkyl,aryl, alkylaryl;

[1998] or

[1999] R(8) and R(9)

[2000] together are part of a 5-, 6- or 7-membered heterocyclic ring;

[2001] A is absent or is a nontoxic organic or inorganic acid;

[2002] (HOE 95/F 109—EP 748 795, NZ 286 583)

[2003] ak) benzyloxycarbonylguanidines of the formula I

[2004] in which:

[2005] R(1), R(2) and R(3)

[2006] independently of one another are —Y-[4-R(8)-phenyl],—Y-[3—R(8)-phenyl] or —Y-[2—R(8)-phenyl],

[2007] where the phenyl is in each case unsubstituted or substituted by1-2 substituents from the group consisting of F, Cl, —CF₃, methyl,hydroxyl, methoxy and —NR(96)R(97);

[2008] R(96) and R(97)

[2009] independently of one another are hydrogen or —CH3;

[2010] Y is a bond, CH₂, oxygen, —S— or —NR(9);

[2011] R(9) is hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[2012] R(8) is SO_(a)[NR(98)]_(b)NR(99)R(10);

[2013] a is 1 or 2;

[2014] b is 0 or 1;

[2015] a+b=2;

[2016] R(98), R(99) and R(10)

[2017]  independently of one another are hydrogen, —(C₁-C₈)-alkyl,benzyl, —(C₂-C₈)-alkylene-NR(11)R(12),(C₂-C₈)-alkylene-NR(13)—(C₂-C₈)-alkylene-NR(37)R(38) or(C₀-C₈)-alkylene-CR(39)R(40)CR(41)R(42)(C₀-C₈)-alkylene-NR(43)R(44);

[2018]  R(11), R(12), R(13), R(37), R(38), R(43) and R(44)

[2019]  independently of one another are hydrogen, —(C₁-C₈)-alkyl orbenzyl;

[2020] R(39), R(40), R(41) and R(42)

[2021]  independently of one another are hydrogen, —(C₁-C₈)-alkyl or—(C₀-C₃)-alkylenephenyl,

[2022]  where the phenyl is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, —CF₃, methyland methoxy;

[2023] or

[2024] R(99) and R(10)

[2025]  together are 4-6 methylene groups, of which one CH₂ group can bereplaced by oxygen, —S—, —NH—, —N—CH₃ or —N-benzyl;

[2026] or

[2027] R(8) is SO_(a)[NR(98)]_(b)NR(95)—C[═N—R(94)]—NR(93)R(92);

[2028] R(92), R(93), R(94) and R(95)

[2029]  independently of one another are hydrogen or alkyl having 1, 2,3 or 4 carbon atoms;

[2030] or

[2031] R(1), R(2) and R(3)

[2032] independently of one another are pyrrol-1-yl, pyrrol-2-yl orpyrrol-3-yl,

[2033] which is not substituted or is substituted by 1-4 substituentsselected from the group consisting of F., Cl, Br, I, —CN,(C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃,methyl, methoxy;

[2034] or

[2035] R(1), R(2) and R(3)

[2036] independently of one another are hydrogen, —(C₁-C₈)-alkyl,—(C₂-C₈)-alkenyl or —(CH₂)_(m)R(14);

[2037] m is zero, 1 or 2;

[2038] R(14) is —(C₃-C₈)-cycloalkyl or phenyl,

[2039] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16);

[2040] R(15) and R(16)

[2041] are hydrogen or —CH₃;

[2042] or

[2043] R(1), R(2) and R(3)

[2044] independently of one another are—Q-4-[(CH₂)_(k)—CHR(17)—(C═O)R(20)]-phenyl,—Q-3-(CH₂)_(k)—CHR(17)—(C═O)R(20)]-phenyl or—Q-2-[(CH₂)_(k)—CHR(17)—(C═O)R(20)]-phenyl,

[2045] where the phenyl in each case is unsubstituted or substituted by1-2 substituents from the group F, Cl, —CF₃, methyl, hydroxyl, methoxyand —NR(35)R(36);

[2046] R(35) and R(36)

[2047] independently of one another are hydrogen or —CH3;

[2048] Q is a bond, oxygen, —S— or —NR(18);

[2049] R(18) is hydrogen or —(C₁-C₄)-alkyl;

[2050] R(17) is —OR(21) or —NR(21)R(22);

[2051] R(21) and R(22)

[2052] independently of one another are hydrogen, —(C₁-C₈)-alkyl,—(C₁-C₈)-alkanoyl, —(C₁-C₈)-alkoxycarbonyl, benzyl, benzyloxycarbonyl;

[2053] or

[2054] R(21) is trityl;

[2055] R(20) is —OR(23) or —NR(23)R(24);

[2056] R(23), R(24) independently of one another are

[2057]  hydrogen, —(C₁-C₈)-alkyl or benzyl;

[2058] k is zero, 1, 2, 3 or 4;

[2059] or

[2060] R(1), R(2) and R(3)

[2061] independently of one another are (C₁-C₉)-heteroaryl,

[2062] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents from the group F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2063] or

[2064] R(1), R(2) and R(3)

[2065] are —SR(25), —OR(25), —NR(25)R(26), —CR(25)R(26)R(27);

[2066] R(25) is —C_(f)H_(2f)—(C₁-C₉)-heteroaryl,

[2067] which is unsubstituted or substituted by 1-3 substituents fromthe group F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino;

[2068] f is zero, 1 or 2;

[2069] R(26) and R(27)

[2070] independently of one another are defined as R(25) or are hydrogenor (C₁-C₄)-alkyl,

[2071] or

[2072] R(1), R(2) and R(3)

[2073] independently of one another are (C₁-C₉)-heteroaryl-N-oxide,

[2074] which is linked via C or N and which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[2075] or

[2076] R(1), R(2) and R(3)

[2077] independently of one another are -SR(28), —OR(28), —NR(28)R(29)or —CR(28)R(29)R(30);

[2078] R(28) is —C_(g)H_(2g)—(C₁-C₉)-heteroaryl-N-oxide,

[2079] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2080] g is zero, 1 or 2;

[2081] R(29), R(30)

[2082] independently of one another are defined as R(28), hydrogen or(C₁-C₄)-alkyl;

[2083] or

[2084] R(1), R(2) and R(3)

[2085] independently of one another are hydrogen, F, Cl, Br, I, —C≡N,T—(CH₂)_(h)—(C_(i)F_(2i+1)), R(31)SO_(l)—R(32)R(33)N—CO—, R(34)—CO— or

[2086] R(45)R(46)N—SO₂, where the perfluoroalkyl group is straight-chainor branched;

[2087] T is a bond, oxygen, —S— or —NR(47);

[2088] l is zero, 1 or 2;

[2089] h is zero, 1 or 2;

[2090] i is 1, 2, 3, 4, 5 or 6;

[2091] R(31), R(32), R(34) and R(45)

[2092] independently of one another are —(C₁-C₈)-alkyl,—(C₃-C₆)-alkenyl, (CH₂)_(n)R(48) or —CF₃;

[2093] n is zero, 1, 2, 3 or 4;

[2094] R(47) is hydrogen or alkyl with 1, 2 or 3 carbon atoms;

[2095] R(48) is —(C₃-C₇)-cycloalkyl or phenyl,

[2096] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, —CF₃, methyl, methoxy and—NR(49)R(50);

[2097] R(49) and R(50)

[2098] are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[2099] or

[2100] R(32), R(34) and R(45)

[2101] are hydrogen;

[2102] R(33) and R(46)

[2103] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2104] or

[2105] R(32) and R(33), and R(45) and R(46)

[2106] together are 5 or 6 methylene groups, of which one CH₂ group canbe replaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[2107] or

[2108] R(1), R(2) and R(3)

[2109] independently of one another are R(51)—A—G—D—;

[2110] R(51) is a basic protonatable radical, i.e. an amino group—NR(52)R(53), an amidino group R(52)R(53)N—C[═N—R(54)]— or a guanidinogroup R(52)R(53)N—C[═N—R(54)]—NR(55)—;

[2111] R(52), R(53), R(54) and R(55)

[2112] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2113] or

[2114] R(52) and R(53) are

[2115] a group C_(α)H_(2α);

[2116] α is 4, 5, 6 or 7;

[2117] where if α=5, 6 or 7 a carbon atom of the group C_(α)H_(2α) canbe replaced by a heteroatom group O, SO_(d) or NR(56),

[2118] or

[2119] R(53) and R(54) or R(54) and R(55) or R(52) and R(55) are

[2120] a group C_(y)H_(2y);

[2121] y is 2, 3, 4 or 5;

[2122] where if y=3, 4 or 5 a carbon atom of the group C_(y)H_(2y) canbe replaced by a heteroatom group O, SO_(d) or NR(56);

[2123] d is zero, 1 or 2;

[2124] R(56) is hydrogen or methyl;

[2125] or

[2126] R(51) is a basic heteroaromatic ring system having 1-9 carbonatoms;

[2127] A is a group C_(e)H_(2e);

[2128] e is zero, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10;

[2129] where in the group C_(e)H_(2e) a carbon atom can be replaced byone of the groupings —O—, —CO—, or —SO_(r)—;

[2130] r is zero, 1 or 2;

[2131] G is a phenylene radical

[2132] R(58) and R(59)

[2133] independently of one another are hydrogen, methyl, methoxy, F,Cl, Br, I, CF₃ or —So_(s)—R(60);

[2134] s zero 1 or 2;

[2135] R(60) is methyl or NR(61)R(62);

[2136]  R(61) and R(62)

[2137]  independently of one another are hydrogen or alkyl having 1, 2,3 or 4 carbon atoms;

[2138] D is —C_(v)H_(2v)—E_(w)—;

[2139] v is zero, 1, 2, 3 or 4;

[2140] E is —O—, —CO—, —CH[OR(63)]—, —SO_(aa)— or —NR(63)—;

[2141] w is zero or 1;

[2142] aa is zero, 1 or 2

[2143] R(63) is hydrogen or methyl,

[2144] or

[2145] R(1), R(2) and R(3)

[2146] independently of one another are —CF₂R(64), —CF[R(65)][R(66)],—CF[(CF₂)_(q)—CF₃)][R(65)], —C[(CF₂)_(p)—CF₃]═CR(65)R(66);

[2147] R(64) is alkyl having 1, 2, 3 or 4 carbon atoms or cycloalkylhaving 3, 4, 5, 6 or 7 carbon atoms;

[2148] R(65) and R(66) independently of one another are hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms;

[2149] q is zero, 1 or 2;

[2150] p is zero, 1 or 2;

[2151] or

[2152] R(1), R(2) and R(3)

[2153] independently of one another are —OR(67) or —NR(67)R(68);

[2154] R(67) and R(68)

[2155] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5 or 6 carbon atoms;

[2156] or

[2157] R(67) and R(68)

[2158] together are 4, 5, 6 or 7 methylene groups, of which one CH₂group can be replaced by oxygen, —S—, SO₂, —NH—, —NCH₃ or —N-benzyl;

[2159] R(4) and R(5)

[2160] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, F, Cl, —OR(69), —NR(70)R(71) or —C_(z)F_(2z+1);

[2161] R(69), R(70) and R(71)

[2162] independently of one another are hydrogen or alkyl having 1, 2 or3 carbon atoms;

[2163] z is 1, 2, 3 or 4;

[2164] R(6) and R(7)

[2165] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2166] X is oxygen or NR(72);

[2167] R(72) is hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[2168] and their pharmaceutically tolerable salts;

[2169] (HOE 95/F 115—EP 744 397, NZ 286 622)

[2170] al) alkenylcarboxylic acid guanidides, carrying fluorophenylgroups, of the Formula I

[2171] in which:

[2172] R(6) is hydrogen, (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl or phenyl,

[2173] where the phenyl group is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(9)R(10);

[2174] R(9) and R(10)

[2175] are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[2176] R(7) independently is defined as R(6);

[2177] R(1), R(2), R(3), R(4) and R(5)

[2178] independently of one another are hydrogen or F;

[2179] where, however, at least one of the radicals R(1), R(2), R(3),R(4) and R(5) must be fluorine;

[2180] and their pharmaceutically tolerable salts;

[2181] (HOE 95/F 167—NZ 299 015)

[2182] am) benzoylguanidines of the formula I

[2183] in which:

[2184] R(1) is R(4)—SO_(m) or R(5)R(6)N—SO₂—;

[2185] m is 1 or 2;

[2186] R(4) and R(5)

[2187] independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms, alkenyl having 3, 4, 5 or 6 carbon atoms, CF₃ or—C_(n)H_(2n)—R(7);

[2188] n is zero, 1, 2, 3 or 4;

[2189] R(6) is H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2190] R(7) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms orphenyl,

[2191] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(8)R(9);

[2192] R(8) and R(9)

[2193]  are H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2194] or

[2195] R(5) is also hydrogen;

[2196] or

[2197] R(5) and R(6)

[2198] together are 4 or 5 methylene groups, of which a CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[2199] or

[2200] R(1) is —O_(p)—(CH₂)_(q)—(CF₂)_(r)—CF₃;

[2201] p is zero or 1;

[2202] q is zero, 1 or 2;

[2203] r is zero, 1, 2 or 3;

[2204] or

[2205] R(1) is —SR(10), —OR(10) or —CR(10)R(11)R(12);

[2206] R(10), R(11) and R(12)

[2207] independently of one another are hydrogen, alkyl having 1, 2, 3,4, 5, 6, 7 or 8 carbon atoms, —C_(s)H_(2s)—(C₃-C₈)-cycloalkyl or anaromatic system selected from the group consisting of pyridyl, pyrrolyl,quinolyl, isoquinolyl, imidazolyl or phenyl;

[2208] s is zero, 1 or 2;

[2209] where the aromatic systems pyridyl, pyrrolyl, quinolyl,isoquinolyl, imidazolyl and phenyl are unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino;

[2210] R(2) is —(CH₂)_(u)—(CF₂)_(t)—CF₃;

[2211] t is zero, 1, 2 or 3;

[2212] u is zero or 1;

[2213] R(3) is hydrogen or independently is defined as R(1);

[2214] and their pharmaceutically tolerable salts;

[2215] (HOE 95/F 173—NZ 299 052)

[2216] an) substituted cinnamic acid guanidides of the formula I

[2217] in which:

[2218] at least one of the substituents R(1), R(2), R(3), R(4) and R(5)is

[2219] —X_(a)—Y_(b)—L_(n)—U;

[2220] X is CR(16)R(17), O, S or NR(18);

[2221] R(16), R(17) and R(18)

[2222] independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2223] a is zero or 1;

[2224] Y is alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkylene-T having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms in the alkylenegroup, T, T-alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms in thealkylene group;

[2225] T is NR(20), O, S or phenylene,

[2226] where the phenylene is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(21)R(22);

[2227] R(20), R(21) and R(22)

[2228]  independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2229] b is zero or 1;

[2230] L is O, S, NR(23) or C_(k)H_(2k);

[2231] k is 1, 2, 3, 4, 5, 6, 7 or 8;

[2232] n is zero or 1;

[2233] U is NR(24)R(25) or an N—containing heterocycle having 1, 2, 3,4, 5, 6, 7, 8 or 9 carbon atoms;

[2234] R(24) and R(25)

[2235] independently of one another are hydrogen, alkyl having 1, 2, 3,4, 5, 6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3, 4, 5, 6,7 or 8 carbon atoms;

[2236] or

[2237] R(24) and R(25)

[2238] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[2239]  where the N-containing heterocycles are N- or C-bridged and arenot substituted or are substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(27)R(28);

[2240] R(23), R(27) and R(28)

[2241] independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2242] and the other substituents R(1), R(2), R(3), R(4) and R(5) ineach case

[2243] independently of one another are H, F, Cl, Br, I, CN,—O_(n)—C_(m)H_(2m+1), —O_(p)—(CH₂)_(s)—C_(q)F_(2q+1) or—C_(r)H_(2r)R(10);

[2244] n is zero or 1;

[2245] m is zero, 1, 2, 3, 4, 5, 6, 7 or 8;

[2246] p is zero or 1;

[2247] q is 1, 2, 3, 4, 5, 6, 7 or 8;

[2248] s is zero, 1, 2, 3 or 4;

[2249] r is zero, 1, 2, 3 or 4;

[2250] R(10)

[2251] is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, or phenyl,

[2252] where the phenyl is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(11)R(12);

[2253] R(11) and R(12)

[2254]  independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2255] R(6) and R(7)

[2256] independently of one another are hydrogen, F, Cl, Br, I, CN,alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, perfluoroalkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5,6, 7 or 8 carbon atoms, or phenyl,

[2257] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(14)R(15);

[2258] R(14) and R(15)

[2259] independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2260] and their pharmaceutically tolerable salts;

[2261] (HOE 95/F 220—NZ 299 052)

[2262] ao) benzoylguanidines of the formula I

[2263] in which:

[2264] at least one of the substituents R(1), R(2) and R(3) isR(6)—C(OH)₂—;

[2265] R(6) is perfluoroalkyl having 1, 2 or 3 carbon atoms, which isstraight-chain or branched;

[2266] and the other substituents R(1), R(2) and R(3)

[2267] independently of one another are hydrogen, OH, F, Cl, Br, I,alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, cycloalkyl having 3, 4, 5or 6 carbon atoms, alkoxy having 1, 2, 3 or 4 carbon atoms, or phenoxy,

[2268] which is unsubstituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, methyl and methoxy;

[2269] or

[2270] the other substituents R(1), R(2) and R(3)

[2271] independently of one another are alkyl-SO_(x), —CR(7)═CR(8)R(9)or —C≡—CR(9);

[2272] x is zero, 1 or 2;

[2273] R(7) is hydrogen or methyl;

[2274] R(8) and R(9)

[2275] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, orphenyl,

[2276] which is unsubstituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl and methoxy;

[2277] or

[2278] the other substituents R(1), R(2) and R(3)

[2279] independently of one another are phenyl, C₈H₅—(C₁-C₄)-alkyl,naphthyl, biphenylyl, quinolinyl, isoquinolinyl or imidazolyl,

[2280] where quinolinyl, isoquinolinyl or imidazolyl are bonded via C orN and where phenyl, C₆H₅-(C₁-C₄)-alkyl, naphthyl, biphenylyl,quinolinyl, isoquinolinyl and imidazolyl are unsubstituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[2281] or

[2282] the other substituents R(1), R(2) and R(3)

[2283] independently of one another are SR(10), —OR(10),—CR(10)R(11)R(12);

[2284] R(10)

[2285] is —C_(f)H_(2f)—(C₃-C₈)-cycloalkyl, quinolinyl, isoquinolinyl,pyridinyl, imidazolyl or phenyl,

[2286] where the aromatic systems quinolinyl, isoquinolinyl, pyridinyl,imidazolyl and phenyl are unsubstituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino;

[2287] f is zero, ₁ or 2;

[2288] R(11) and R(12)

[2289] independently of one another are defined as R(10), hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms;

[2290] R(4) and R(5)

[2291] independently of one another are hydrogen, alkyl having 1, 2 or 3carbon atoms, F, Cl, Br, I, CN, OR(13), NR(14)R(15),—(CH₂)_(n)—(CF₂)_(o)—CF₃;

[2292] R(13), R(14) and R(15)

[2293] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2294] n is zero or 1;

[2295] o is zero, 1 or 2;

[2296] and their pharmacologically acceptable salts;

[2297] (HOE 95/F 253—NZ 299 682)

[2298] ap) sulfonimidamides of the formula I

[2299] in which:

[2300] at least one of the three substituents R(1), R(2) and R(3) is abenzoylguanidine,

[2301] which is unsubstituted or substituted in the phenyl moiety by 1-4radicals selected from the group consisting of alkyl having 1, 2, 3, 4,5, 6, 7 or 8 carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbonatoms, —(CH₂)_(m)—R(14), F, Cl, Br, I, —C≡N, CF₃, R(22)SO₂—,R(23)R(24)N—CO—, R(25)—CO—,

[2302] R(26)R(27)N—SO₂, —OR(35), —SR(35) or —NR(35)R(36);

[2303] m is zero, 1 or 2;

[2304] R(14)

[2305] is —(C₃-C₈)-cycloalkyl or phenyl,

[2306] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16);

[2307] R(15) and R(16)

[2308]  independently of one another are hydrogen or —CH₃;

[2309] R(22), R(23), R(25) and R(26)

[2310] independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms,(CH₂)_(n)R(29) or —CF₃;

[2311] n is zero, 1, 2, 3 or 4;

[2312] R(29) is —(C₃-C₇)-cycloalkyl or phenyl,

[2313] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, —CF₃, methyl, methoxy and—NR(30)R(31);

[2314] R(30) and R(31)

[2315] are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[2316] or

[2317] R(23), R(25) and R(26)

[2318] are hydrogen;

[2319] R(24) and R(27)

[2320] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2321] or

[2322] R(23) and R(24), and also R(26) and R(27)

[2323] together are 5 or 6 methylene groups, of which one CH₂ group canbe replaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[2324] R(35) and R(36)

[2325] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5 or 6 carbon atoms;

[2326] or

[2327] R(35) and R(36)

[2328] together are 4-7 methylene groups, of which one CH₂ group can bereplaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[2329] or

[2330] R(35) is phenyl,

[2331] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, —CF₃, methyl, methoxy,SO₂R(5), SO₂NR(6)R(7) and —NR(32)R(33);

[2332] R(5) is alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms;

[2333] R(6) and R(7)

[2334] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2335] R(32) and R(33)

[2336] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2337] or

[2338] R(35) is C₁-C₉-heteroaryl,

[2339] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2340] and the other substituents R(1), R(2) and R(3) in each case

[2341] independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms, (CH₂)_(p)R(10);

[2342] p is zero, 1, 2, 3 or 4;

[2343] R(10) is phenyl,

[2344] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, —CF₃, methyl, methoxy,—SO₂NR(17)R(8) and —SO₂R(9);

[2345] R(17) and R(8)

[2346] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2347] R(9) is alkyl having 1, 2, 3 or 4 carbon atoms;

[2348] or

[2349] the other radical R(1) or R(3) in each case

[2350] is hydrogen,

[2351] R(4) is hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[2352] and their pharmaceutically tolerable salts;

[2353] (HOE 95/F 265—NZ 299 739)

[2354] aq) benzoylguanidines of the formula I

[2355] in which:

[2356] R(1) is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms orNR(7)R(8);

[2357] R(7) and R(8)

[2358] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5, 6, 7 or 8 carbon atoms;

[2359] R(2) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms or —SO₂R(9);

[2360] R(9) independently is defined as R(1);

[2361] R(3) is hydrogen, —SR(25), —OR(25), —NR(25)R(26) or—CR(25)R(26)R(27);

[2362] R(25) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, or phenyl,

[2363] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2364] or

[2365] R(25)

[2366] is —(C₁-C₉)-heteroaryl,

[2367] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2368] R(26) and R(27)

[2369] independently of one another are defined as R(25) or are hydrogenor alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;

[2370] R(4) is hydrogen, F, Cl, Br, I, OH, —C≡N, CF₃, alkyl having 1, 2,3, 4, 5, 6, 7 or 8 carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8carbon atoms or —(CH₂)_(m)R(14);

[2371] m is zero, 1 or 2;

[2372] R(14) is —(C₃-C₈)-cycloalkyl or phenyl,

[2373] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16);

[2374] R(15) and R(16)

[2375] independently of one another are hydrogen or —CH₃;

[2376] R(5) and R(6)

[2377] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, F, Cl, —OR(32), —NR(33)R(34) or CF₃;

[2378] R(32), R(33) and R(34)

[2379] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2380] and their pharmaceutically tolerable salts;

[2381] (HOE 95/F 269 K—EP-A 774 458)

[2382] ar) benzenedicarboxylic acid diguanidides of the formula I

[2383] in which:

[2384] one of the radicals R(1), R(2), R(3) and R(4)

[2385] is —CO—N═C(NH₂)₂;

[2386] and of the other radicals R(1), R(2), R(3) and R(4) in each case:

[2387] R(1) is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, F, Cl,Br, I, —OR(32), —NR(33)R(34) or CF₃;

[2388] R(32), R(33) and R(34)

[2389] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2390] R(2) and R(4)

[2391] independently of one another are hydrogen, F, Cl, Br, I, OH, —CN,CF₃, —CO—N═C(NH₂)₂, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms or —(CH₂)_(m)R(14);

[2392] m is zero, 1 or 2;

[2393] R(14) is —(C₃-C₈)-cycloalkyl or phenyl,

[2394] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16);

[2395] R(15) and R(16)

[2396] are hydrogen or —CH₃;

[2397] or

[2398] R(2) and R(4)

[2399] independently of one another are pyrrol-1-yl, pyrrol-2-yl orpyrrol-3-yl,

[2400] which is not substituted or is substituted by 1-4 substituentsselected from the group consisting of F, Cl, Br, 1, —CN,(C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃,methyl, methoxy;

[2401] or

[2402] R(2) and R(4)

[2403] independently of one another are R(22)—SO₂—, R(23)R(24)N—CO—,R(28)—CO— or R(29)R(30)N—SO₂;

[2404] R(22) and R(28)

[2405] independently of one another are methyl or —CF₃;

[2406] R(23), R(24), R(29) and R(30)

[2407] independently of one another are hydrogen or methyl;

[2408] or

[2409] R(2) and R(4)

[2410] independently of one another are —OR(35) or —NR(35)R(36);

[2411] R(35) and R(36)

[2412] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5 or 6 carbon atoms;

[2413] or

[2414] R(35) and R(36)

[2415] together are 4-7 methylene groups, of which one CH₂ group can bereplaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[2416] R(3) is hydrogen, —SR(25), —OR(25), —NR(25)R(26),—CR(25)R(26)R(27);

[2417] R(25) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms or phenyl,

[2418] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2419] or

[2420] R(25) is —(C₁-C₉)-heteroaryl,

[2421] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2422] R(26) and R(27)

[2423] independently of one another are defined as R(25) or are hydrogenor alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;

[2424] R(5) is alkyl having 1, 2, 3 or 4 carbon atoms, F, Cl, Br, I,X—(CH₂)_(y)—CF₃ or phenyl,

[2425] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(6)R(7);

[2426] R(6) and R(7)

[2427] independently of one another are hydrogen or —CH₃;

[2428] X is a bond or oxygen;

[2429] y is zero, 1 or 2;

[2430] and their pharmaceutically tolerable salts;

[2431] (HOE 95/F 269 BK—EP-A 774 457)

[2432] as) benzenedicarboxylic acid diguanidides of the formula I

[2433] in which:

[2434] one of the radicals R(1), R(2), R(3) and R(5)

[2435] is —CO—N═C(NH₂)₂;

[2436] and of the other radicals R(1), R(2), R(3) and R(5) in each case:

[2437] R(1) and R(5)

[2438] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, F, Cl, —OR(32), —NR(33)R(34) or CF₃;

[2439] R(32), R(33) and R(34)

[2440] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2441] R(2) is hydrogen, F, Cl, Br, I, OH, —CN, CF₃, —CO—N═C(NH₂)₂,alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, alkenyl having 2, 3,4, 5, 6, 7 or 8 carbon atoms or —(CH₂)_(m)R(14);

[2442] m is zero, 1 or 2;

[2443] R(14) is —(C₃-C₈)-cycloalkyl or phenyl,

[2444] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16);

[2445] R(15) and R(16)

[2446] independently of one another are hydrogen or —CH₃;

[2447] or

[2448] R(2) is R(22)—SO₂—, R(23)R(24)N—CO—, R(28)—CO— orR(29)R(30)N—SO₂;

[2449] R(22) and R(28)

[2450] independently of one another are methyl or —CF₃;

[2451] R(23), R(24), R(29) and R(30)

[2452] independently of one another are hydrogen or methyl;

[2453] or

[2454] R(2) is —OR(35) or —NR(35)R(36);

[2455] R(35) and R(36)

[2456] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5 or 6 carbon atoms;

[2457] or

[2458] R(35) and R(36)

[2459] together are 4-7 methylene groups, of which one CH₂ group can bereplaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[2460] R(3) is hydrogen, —SR(25), —OR(25), —NR(25)R(26),—CR(25)R(26)R(27);

[2461] R(25) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, or phenyl,

[2462] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2463] or

[2464] R(25) is —(C₁-C₉)-heteroaryl,

[2465] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2466] R(26) and R(27)

[2467] independently of one another are defined as R(25) or are hydrogenor alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;

[2468] R(4) is CF₃, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms, —(C₃-C₈)-cycloalkylor —(CH₂)_(m)R(14);

[2469] m is 1 or 2;

[2470] R(14) is —(C₃-C₈)-cycloalkyl or phenyl,

[2471] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16);

[2472] R(15) and R(16)

[2473] independently of one another are hydrogen or —CH₃;

[2474] or

[2475] R(4) is phenyl,

[2476] which is substituted by 2, 3, 4 or five substituents selectedfrom the group consisting of F, Cl, CF₃, methyl, methoxy and—NR(15)R(16);

[2477] R(15) and R(16)

[2478] independently of one another are hydrogen or CH₃;

[2479] and their pharmaceutically tolerable salts;

[2480] (HOE 96/F 013—EP-A 787 717)

[2481] at) diaryldicarboxylic acid diguanidides of the formula I

[2482] in which:

[2483] one of the radicals R(1), R(2), R(3), R(4) and R(5)

[2484] is —CO—N═C(NH₂)₂;

[2485] the other radicals R(1) and R(5) in each case

[2486] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, F, Cl, —OR(32), —NR(33)R(34) or CF₃;

[2487] R(32), R(33) and R(34)

[2488] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2489] the other radicals R(2) and R(4) in each case

[2490] independently of one another are hydrogen, F, Cl, Br, I, OH, —CN,CF₃, —CO—N═C(NH₂)₂, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms or —(CH₂)_(m)R(14);

[2491] m is zero, 1 or 2;

[2492] R(14) is —(C₃-C₈)-cycloalkyl or phenyl,

[2493] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16);

[2494] R(15) and R(16)

[2495] are hydrogen or —CH₃;

[2496] or

[2497] the other radicals R(2) and R(4) in each case

[2498] independently of one another are pyrrol-1-yl, pyrrol-2-yl orpyrrol-3-yl,

[2499] which is not substituted or is substituted by 1-4 substituentsselected from the group consisting of F, Cl, Br, 1, —CN,(C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃,methyl, methoxy;

[2500] or

[2501] the other radicals R(2) and R(4) in each case

[2502] are R(22)—SO₂—, R(23)R(24)N—CO—, R(28)—CO— or R(29)R(30)N—SO₂;

[2503] R(22) and R(28)

[2504] independently of one another are methyl or —CF₃;

[2505] R(23), R(24), R(29) and R(30)

[2506] independently of one another are hydrogen or methyl;

[2507] or

[2508] the other radicals R(2) and R(4) in each case

[2509] independently of one another are —OR(35) or —NR(35)R(36);

[2510] R(35) and R(36)

[2511] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5 or 6 carbon atoms;

[2512] or

[2513] R(35) and R(36)

[2514] together are 4-7 methylene groups, of which one CH₂ group can bereplaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[2515] the other radical R(3) in each case

[2516] is hydrogen, —SR(25), —OR(25), —NR(25)R(26), —CR(25)R(26)R(27);

[2517] R(25) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, or phenyl,

[2518] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2519] or

[2520] R(25) is —(C₁-C₉)-heteroaryl,

[2521] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F. Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2522] R(26) and R(27)

[2523] independently of one another are defined as R(25) or are hydrogenor alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;

[2524] one of the radicals R(6), R(7), R(8), R(9) and R(10)

[2525] is —CO—N═C(NH₂)₂;

[2526] the other radicals R(6) and R(10) in each case

[2527] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, F, Cl, —OR(132), —NR(133)R(134) or CF₃;

[2528] R(132), R(133) and R(134)

[2529] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2530] the other radicals R(7) and R(9) in each case

[2531] independently of one another are hydrogen, F, Cl, Br, I, OH, —CN,CF₃, —CO—N═C(NH₂)₂, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms or —(CH₂)_(mm)R(114);

[2532] mm is zero, 1 or 2;

[2533] R(114)

[2534] is —(C₃-C₈)-cycloalkyl or phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of Fand Cl, —CF₃, methyl, methoxy and —NR(115)R(116);

[2535] R(115) and R(116)

[2536]  are hydrogen or —CH₃;

[2537] or

[2538] the other radicals R(7) and R(9) in each case

[2539] independently of one another are pyrrol-1-yl, pyrrol-2-yl orpyrrol-3-yl,

[2540] which is not substituted or is substituted by 1-4 substituentsselected from the group consisting of F, Cl, Br, I, —CN,(C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃, methyland methoxy;

[2541] or

[2542] the other radicals R(7) and R(9) in each case

[2543] are R(122)-SO₂—, R(123)R(124)N—CO—, R(128)—CO— or

[2544] R(129)R(130)N—SO₂;

[2545] R(122) and R(128)

[2546] independently of one another are methyl or —CF₃;

[2547] R(123), R(124), R(129) and R(130)

[2548] independently of one another are hydrogen or methyl;

[2549] or

[2550] the other radicals R(7) and R(9) in each case

[2551] independently of one another are —OR(135) or —NR(135)R(136);

[2552] R(135) and R(136)

[2553] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5 or 6 carbon atoms;

[2554] or

[2555] R(135) and R(136)

[2556] together are 4-7 methylene groups, of which one CH₂ group can bereplaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;

[2557] the other radical R(8) in each case

[2558] is hydrogen, —SR(125), —OR(125), —NR(125)R(126) or—CR(125)R(126)R(127);

[2559] R(125)

[2560] is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atomsor phenyl,

[2561] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2562] or

[2563] R(125)

[2564] is —(C₁-C₉)-heteroaryl,

[2565] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2566] R(126) and R(127)

[2567] independently of one another are defined as R(125) or arehydrogen or alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;

[2568] A is absent or is —NR(11)—CO—, —NR(12)—CO—NR(13)—,—NR(17)—CO—NR(18)—SO₂—, —NR(19)—SO₂—, —SO₂—NR(19)—SO₂—, —SO₂—NR(19)—CO—,—O—CO—NR(19)—SO₂— or —CR(20)═CR(21)—;

[2569] R(11), R(12), R(13), R(17), R(18), R(19), R(20) and R(21)

[2570] independently of one another are hydrogen or alkyl having 1, 2,3, 4, 5, 6, 7 or 8 carbon atoms

[2571] and their pharmaceutically tolerable salts;

[2572] (HOE 96/F 026—EP-A 790 245)

[2573] au) substituted thiophenylalkenylcarboxylic acid guanidides ofthe formula I

[2574] in which:

[2575] at least one of the substituents R(1), R(2) and R(3)

[2576] is —O_(p)—(CH₂)_(s)—C_(q)F_(2q+1), R(40)CO— or R(³¹)SO_(k)—;

[2577] p is zero or 1;

[2578] s is zero, 1, 2, 3 or 4;

[2579] q is 1, 2, 3, 4, 5, 6, 7 or 8;

[2580] k is zero, 1 or 2;

[2581] R(40) is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,

[2582] perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, or phenyl,

[2583] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl and methoxy;

[2584] R(31) is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkylhaving 3, 4, 5, 6, 7 or 8 carbon atoms, or phenyl,

[2585] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl or methoxy;

[2586] or

[2587] R(31) is NR(41)R(42);

[2588] R(41) and R(42)

[2589] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms,

[2590] or

[2591] R(41) and R(42)

[2592] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[2593] and the other substituents R(1), R(2) and R(3) in each case

[2594] independently of one another are H, F, Cl, Br, I, CN,—O_(na)—C_(ma)H_(2ma+1)

[2595] or —O_(ga)C_(ra)H_(2ra)R(10);

[2596] na is zero or 1;

[2597] ma is zero, 1, 2, 3, 4, 5, 6, 7 or 8;

[2598] ga is zero or 1;

[2599] ra is zero, 1, 2, 3 or 4;

[2600] R(10) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms orphenyl,

[2601] where the phenyl is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyland methoxy;

[2602] R(4) and R(5)

[2603] independently of one another are hydrogen, F, Cl, Br, I, CN,alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, perfluoroalkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5,6, 7 or 8 carbon atoms or phenyl,

[2604] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(14)R(15);

[2605] R(14) and R(15)

[2606] independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfl.uoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2607] and their pharmaceutically tolerable salts;

[2608] (HOE 96/F 032—EP-A 791 557)

[2609] av) ortho-substituted benzoylguanidines of the formula I

[2610] in which:

[2611] R(2) and R(3)

[2612] independently of one another are hydrogen, Cl, Br, I,(C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl or —OR(5);

[2613] R(5) is (C₁-C₈)-alkyl or —C_(d)H_(2d)—(C₃-C₈)-cycloalkyl;

[2614] d is zero, 1 or 2;

[2615] where one of the two substituents R(2) and R(3) is alwayshydrogen but both substituents R(2) and R(3) are not simultaneouslyhydrogen,

[2616] and their pharmaceutically tolerable salts;

[2617] (HOE 96/F 042—EP-A 794 171)

[2618] aw) benzoylguanidines of the formula I

[2619] in which:

[2620] R(1) is H, F, Cl, Br, I, CN, NO₂, alkyl having 1, 2, 3, 4, 5, 6,7 or 8 carbon atoms, alkoxy having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkoxyhaving 3, 4, 5, 6, 7 or 8 carbon atoms or X_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃;

[2621] X is oxygen, S, NR(5),

[2622] a is zero or 1;

[2623] b is zero, 1 or 2;

[2624] c is zero, 1, 2 or 3;

[2625] R(5) is H, alkyl having 1, 2, 3 or 4 carbon atoms or—C_(d)H_(2d)R(6);

[2626] d is zero, 1, 2, 3 or 4;

[2627] R(6) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms,phenyl, biphenylyl or naphthyl,

[2628]  where the aromatics phenyl, biphenylyl or naphthyl are notsubstituted or are substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(7)R(8);

[2629]  R(7) and R(8)

[2630]  independently are H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2631] or

[2632] R(1) is —SR(10), —OR(10) or —CR(10)R(11)R(12);

[2633] R(10) is —C_(f)H₂f-cycloalkyl having 3, 4, 5, 6, 7 or 8 carbonatoms in the cycloalkyl ring, or phenyl,

[2634] where phenyl is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2635] f is zero, 1 or 2;

[2636] R(11) and R(12)

[2637] independently of one another are defined as R(10) or are hydrogenor alkyl having 1, 2, 3 or 4 carbon atoms;

[2638] or

[2639] R(1) is phenyl, naphthyl, biphenylyl or heteroaryl having 1, 2,3, 4, 5, 6, 7, 8 or 9 carbon atoms, with the latter being linked via acarbon atom or a nitrogen atom of the ring,

[2640] which are in each case unsubstituted or substituted by 1-3substituents selected from the group consisting of F, CI, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino,

[2641] or

[2642] R(1) is —SR(13), —OR(13), —NHR(13), —NR(13)R(14), —CHR(13)R(15),—C[R(15)R(16)OH], —C≡CR(18), —C[R(19)]═CHR(18),—C[R(20)R(21)]_(k)—(CO)—[CR(22)R(23)]_(l)—R(24),

[2643] k is zero, 1, 2, 3 or 4;

[2644] l is zero, 1, 2, 3 or 4;

[2645] R(13) and R(14)

[2646] identically or differently are—(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(j)—R(17) or—(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(24); R(17) is hydrogen or methyl,

[2647] g, h and i

[2648] identically or differently are zero, 1, 2, 3 or 4;

[2649] j is 1, 2, 3 or 4;

[2650] R(15) and R(16)

[2651] identically or differently are hydrogen, alkyl having 1, 2, 3, 4,5 or 6 carbon atoms or, together with the carbon atom carrying them, arecycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms;

[2652] R(18)

[2653] is phenyl,

[2654] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(25)R(26);

[2655] R(25) and R(26)

[2656]  are H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2657] or

[2658] R(18) is heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms,

[2659] which is unsubstituted or substituted as phenyl;

[2660] or

[2661] R(18) is alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,

[2662] which is unsubstituted or substituted by 1-3 OH;

[2663] or

[2664] R(18)

[2665] is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms;

[2666] R(19), R(20), R(21), R(22) and R(23)

[2667] identically or differently are hydrogen or methyl;

[2668] R(24) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(m)H₂m—R(18);

[2669] m is 1, 2, 3 or 4;

[2670] R(2) and R(3)

[2671] are defined as R(1);

[2672] R(4) is alkyl having 1, 2, 3 or 4 carbon atoms;

[2673] and their pharmaceutically tolerable salts;

[2674] (HOE 96/F 043—EP-A 794 172)

[2675] ax) ortho-substituted benzoylguanidines of the formula I

[2676] in which:

[2677] R(1) is H, F, Cl, Br, I, CN, NO₂, alkyl having 1, 2, 3, 4, 5, 6,7 or 8 carbon atoms, alkoxy having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkoxyhaving 3, 4, 5, 6, 7 or 8 carbon atoms or X_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃;

[2678] X is oxygen, S, NR(5),

[2679] a is zero or 1;

[2680] b is zero, 1 or 2;

[2681] c is zero, 1, 2 or 3;

[2682] R (5) is H, alkyl having 1, 2, 3 or 4 carbon atoms or—C_(d)H_(2d)R(6);

[2683] d is zero, 1, 2, 3 or 4;

[2684] R(6) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms,phenyl, biphenylyl or naphthyl,

[2685]  where the aromatics phenyl, biphenylyl or naphthyl are notsubstituted or are substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(7)R(8);

[2686]  R(7) and R(8)

[2687]  independently are H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2688] or

[2689] R(1) is —SR(10), —OR(10) or —CR(10)R(11)R(12);

[2690] R(10) is —C_(f)H_(2f)-cycloalkyl having 3, 4, 5, 6, 7 or 8 carbonatoms in the cycloalkyl ring, or phenyl,

[2691] where phenyl is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2692] f is zero, 1 or 2;

[2693] R(11) and R(12)

[2694] independently of one another are defined as R(10), or arehydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[2695] or

[2696] R(1) is phenyl, naphthyl, biphenylyl or heteroaryl having 1, 2,3, 4, 5, 6, 7, 8 or 9 carbon atoms, with the latter being linked via acarbon atom or a nitrogen atom of the ring,

[2697] which are in each case unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylarnino,

[2698] or

[2699] R(1) is —SR(13), —OR(13), —NHR(13), —NR(13)R(14), —CHR(13)R(15),—C[R(15)R(16)OH], —C≡CR(18), —C[R(19)]=CHR(18),—C[R(20)R(21)]_(k)—(CO)—[CR(22)R(23)]_(l)—R(24),

[2700] k is zero, 1, 2, 3 or 4;

[2701] l is zero, 1, 2, 3 or 4;

[2702] R(13) and R(14)

[2703] identically or differently are—(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(j)—R(17) or—(CH₂)_(g)—O—(CH₂—CH₂₀)_(h)—R(24);

[2704] R(17) is hydrogen or methyl,

[2705] g, h and i

[2706] identically or differently are zero, 1, 2, 3 or 4;

[2707] is 1, 2, 3 or 4;

[2708] R(15) and R(16)

[2709] identically or differently are hydrogen, alkyl having 1, 2, 3, 4,5 or 6 carbon atoms or, together with the carbon atom carrying them, arecycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms;

[2710] R(18)

[2711] is phenyl,

[2712] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(25)R(26);

[2713] R(25) and R(26)

[2714]  are H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2715] or

[2716] R(18) is heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms,

[2717] which is unsubstituted or substituted as phenyl;

[2718] or

[2719] R(18) is alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,

[2720] which is unsubstituted or substituted by 1-3 OH;

[2721] or

[2722] R(18)

[2723] is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms;

[2724] R(19), R(20), R(21), R(22) and R(23)

[2725] identically or differently are hydrogen or methyl;

[2726] R(24) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(m)H_(2m)—R(18);

[2727] m is 1, 2, 3 or 4;

[2728] one of the two substituents R(2) and R(3)

[2729] is hydroxyl;

[2730] and

[2731] the other of the substituents R(2) and R(3) in each case

[2732] is defined as R(1);

[2733] R(4) is alkyl having 1, 2, 3 or 4 carbon atoms; alkoxy having 1,2, 3 or 4 carbon atoms, F, Cl, Br, I or —(CH₂)_(n)—(CF₂)_(o)—CF₃;

[2734] n is zero or 1;

[2735] o is zero or 1;

[2736] and their pharmaceutically tolerable salts;

[2737] (HOE 96/F 135—EP-A 810 207)

[2738] ay) bis-ortho-substituted benzoylguanidines of the formula I

[2739] in which:

[2740] R(1), R(2) and R(3)

[2741] independently of one another are R(10)—SO_(a)— orR(14)R(15)N—SO₂—;

[2742] a is zero, 1 or 2,

[2743] R(10), R(14) and R(15)

[2744] independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms, perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, alkenyl having 3, 4, 5 or 6 carbon atoms or —C_(ab)H_(2ab)—R(16);

[2745] ab is zero, 1, 2, 3 or 4;

[2746] R(16) is cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms, orphenyl,

[2747] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃₁ methyl, methoxy andNR(17)R(18);

[2748] R(17) and R(18)

[2749]  independently of one another are hydrogen, CF₃ or alkyl having1, 2, 3 or 4 carbon atoms;

[2750] or

[2751] R(14) and R(15)

[2752] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[2753] or

[2754] R(14) and R(15)

[2755] are hydrogen;

[2756] or

[2757] R(1), R(2) and R(3)

[2758] independently of one another are SR(21), —OR(22), —NR(23)R(24) or—CR(25)R(26)R(27);

[2759] R(21), R(22), R(23) and R(25)

[2760] independently of one another are —C_(b)H_(2b)—(C₁-C₉)-heteroaryl,

[2761] which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃₁ CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino;

[2762] b is zero, 1 or 2;

[2763] R(24), R(26) and R(27)

[2764] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2765] or

[2766] R(1), R(2) and R(3)

[2767] independently of one another are hydrogen, F, Cl, Br, I, CN,—(Xa)_(dg)—C_(da)H_(2da+1), —(Xb)_(dh)—(CH₂)_(db)—C_(de)F_(2de+1),alkenyl having 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(df)H_(2df)R(³⁰);

[2768] (Xa) is oxygen, sulfur or NR(33);

[2769] R(33) is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms or

[2770] perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2771] dg is zero or 1;

[2772] (Xb) is oxygen, sulfur or NR(34);

[2773] R(34) is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms orperfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2774] dh is zero or 1;

[2775] da is zero, 1, 2, 3, 4, 5, 6, 7 or 8;

[2776] db is zero, 1, 2, 3 or 4;

[2777] de is zero, 1, 2, 3, 4, 5, 6 or 7;

[2778] df is zero, 1, 2, 3 or 4;

[2779] R(30) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms,phenyl, biphenylyl or naphthyl,

[2780] where the aromatics phenyl, biphenylyl and naphthyl are notsubstituted or are substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(31)R(32);

[2781] R(31) and R(32)

[2782]  are hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms orperfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2783] or

[2784] R(1), R(2) and R(3)

[2785] independently of one another are NR(40)R(41) or—(Xe)—(CH₂)_(eb)R(45);

[2786] R(40) and R(41)

[2787] independently of one another are hydrogen, alkyl having 1, 2, 3,4, 5, 6, 7 or 8 carbon atoms, perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms or (CH₂)_(e)—R(42);

[2788] e is zero, 1, 2, 3 or 4;

[2789] R(42) is cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms orphenyl,

[2790] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy and

[2791] NR(43)R(44);

[2792] R(43) and R(44)

[2793]  independently of one another are hydrogen, CF₃ or alkyl having1, 2, 3 or 4 carbon atoms;

[2794] or

[2795] R(40) and R(41)

[2796] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[2797] (Xe) is oxygen, sulfur or NR(47);

[2798] R(47) is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms orperfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2799] eb is zero, 1, 2, 3 or 4;

[2800] R(45) is cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms, orphenyl,

[2801] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy,NR(50)R(51) and —(Xfa)—(CH₂)_(ed)—(Xfb)R(46);

[2802] Xfa is CH₂, oxygen, sulfur or NR(48);

[2803] Xfb is oxygen, sulfur or NR(49);

[2804] R(48), R(49), R(50) and R(51)

[2805]  independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2806] ed is 1, 2, 3 or 4;

[2807] R(46) is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms orperfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2808] or

[2809] R(1), R(2) and R(3)

[2810] independently of one another are —CHR(52)R(53);

[2811] R(52) is —(CH₂)_(g)—(CHOH)_(h)—(CH)_(i)—(CHOH)_(k)—R(54) or—(CH₂)_(g)—O—(CH₂-CH₂O)_(h)—R(54);

[2812] R(54) is hydrogen or methyl;

[2813] g, h, i

[2814] identically or differently are zero, 1, 2, 3 or 4;

[2815] k is 1, 2, 3 or 4;

[2816] R(53) is hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;

[2817] or

[2818] R(1), R(2) and R(3)

[2819] independently of one another are —C(OH)R(55)R(56);

[2820] R(55) and R(56)

[2821] identically or differently are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[2822] or

[2823] R(55) and R(56)

[2824] together are cycloalkyl having 3, 4, 5 or 6 carbon atoms;

[2825] or

[2826] R(55) is —CH₂OH;

[2827] and

[2828] R(4) and R(5)

[2829] independently of one another are alkyl having 1, 2, 3 or 4 carbonatoms, alkoxy having 1, 2, 3 or 4 carbon atoms, OH, F, Cl, Br, I, CN,—O_(n)—(CH₂)_(o)—(CF₂)_(p)—CF₃;

[2830] n is zero or 1;

[2831] o is zero, 1 or 2;

[2832] p is zero, 1 or 2;

[2833] and their pharmaceutically tolerable salts;

[2834] (96/F 136—EP-A 810 205)

[2835] az) substituted 1-naphthoylguanidines of the formula I

[2836] in which:

[2837] R2, R3, R4, R5, R6, R7 and R8

[2838] independently of one another are H, F, Cl, Br, I, CN, NO₂, CF₃,C₂F5 or X_(a)Y_(b)Z;

[2839] X is O, S, NR(10), CR(11)R(12), C═O, C(═O)NR(10), C(═O)O, SO,SO₂, SO₂NR(10), OC═O, NR(10)C═O or NR(10)SO₂,

[2840] where the linkage with the naphthalene ring in each case takesplace via the left atom;

[2841] R(10), R(11) and R(12)

[2842] independently of one another are H, alkyl having 1, 2, 3, 4, 5 or6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms orcycloalkyl having 3, 4, 5, 6 or 7 carbon atoms;

[2843] a is zero or 1;

[2844] Y is alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 CH₂ groups,

[2845] where one of these CH₂ groups can be replaced by O, S, NR(13) oro-, p- or m-phenylene;

[2846] R(13) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5 or 6 carbon atoms;

[2847] b is zero or 1;

[2848] Z is H, alkyl having 1, 2, 3, 4, 5, 6 or 7 carbon atoms,cycloalkyl

[2849] having 3, 4, 5, 6 or 7 carbon atoms, C(═O)R(15), SO₂R(15),

[2850] NR(16)R(17) or phenyl,

[2851] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, Br, CF₃, methyl, methoxyand NR(21)R(22);

[2852] R(21) and R(22)

[2853] independently of one another are H or alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2854] R(15) is N═C(NH₂)₂, NR(18)R(19), N(CH₂)_(c)NR(18)R(19) or OR(20);

[2855] c is 2 or 3;

[2856] R(18) and R(19)

[2857] independently of one another are H, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms;

[2858] or

[2859] R(18) and R(19)

[2860] together are 4 or 5 methylene groups,

[2861]  of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chlorophenyl);

[2862] R(20) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5, 6 or 7 carbon atoms;

[2863] R(16) and R(17)

[2864] independently of one another are H, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms;

[2865] or

[2866] R(16) and R(17)

[2867] together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃, N-benzyl or N-(p-chlorophenyl);

[2868] or

[2869] Z is an N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or9 carbon atoms,

[2870] where the N-containing heterocycle is linked via N or C and isnot substituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, Br, CF₃, methyl, methoxy and NR(21)R(22);

[2871] but where, in the case where R(4) is an alkoxy radical, at leastone of the substituents R(2), R(3), R(5), R(6), R(7) and R(8) is nothydrogen;

[2872] and their pharmaceutically tolerable salts;

[2873] (96/F 137—EP-A 810 206)

[2874] ba) substituted 2-naphthoylguanidines of the formula I

[2875] in which:

[2876] at least one of the substituents R1, R3, R4, R5, R6, R7 and R8 is

[2877] XY_(a)WZ or X′Y_(a)WZ′;

[2878] X is O, S, NR(10) or CR(11)R(12);

[2879] R(10), R(11) and R(12)

[2880] independently of one another are H, alkyl having 1, 2, 3, 4, 5 or6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms orcycloalkyl having 3, 4, 5, 6 or 7 carbon atoms;

[2881] Y is alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 CH₂ groups,

[2882] where one of these CH₂ groups can be replaced by O, S, NR(13) oro-, p- or m-phenylene;

[2883] R(13) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5 or 6 carbon atoms;

[2884] a is zero or 1;

[2885] W is CH₂, SO₂, S(═O)(═NH) or—if W does not immediately follow aheteroatom of the group XY_(a)—alternatively O or NR(14);

[2886] R(14) is H, alkyl having 1, 2, 3, 4, 5 or —6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5 or 6 carbon atoms;

[2887] Z is C(═O)R(15), SO₂R(15) or—if W is not O or—NR(14)—alternatively NR(16)R(17);

[2888] R(15) is N═C(NH₂)₂, NR(18)R(19), N(CH₂)bNR(18)R(19) or OR(20);

[2889] b is 2 or 3;

[2890] R(18) and R(19)

[2891]  independently of one another are H, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms;

[2892] or

[2893] R(18) and R(19)

[2894]  together are 4 or 5 methylene groups,

[2895]  of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chlorophenyl);

[2896] R(20) is

[2897]  H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3, 4, 5, 6 or 7carbon atoms;

[2898] R(16) and R(17)

[2899] independently of one another are H, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms;

[2900] or,

[2901] R(16) and R(17)

[2902] together are 4 or 5 methylene groups,

[2903]  of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chlorophenyl);

[2904] X′ is C═O, C(═O)NR(30), C(═O)O, SO, SO₂, SO₂NR(30), OC═O,NR(30)C═O or NR(30)SO₂,

[2905] where the linkage with the naphthalene ring in each case takesplace via the left atom;

[2906] R(30) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5, 6 or 7 carbon atoms;

[2907] Z′ is C(═O)R(15), SO₂R(15), an N-containing heterocycle having 1,2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms,

[2908] where the N-containing heterocycle is linked via N or C and isnot substituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, Br, CF₃, methyl, methoxy and NR(21)R(22);

[2909] R(21) and R(22)

[2910] independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2911] R(15) is N═C(NH₂)₂, NR(18)R(19), N(CH₂)_(b)NR(18)R(19) or OR(20);

[2912] R(18) and R(19)

[2913]  independently of one another are H, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms;

[2914] or

[2915] R(18) and R(19)

[2916]  together are 4 or 5 methylene groups,

[2917]  of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chlorophenyl);

[2918] b is 2 or 3;

[2919] R(20) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5, 6 or 7 carbon atoms;

[2920] or

[2921] Z′—if W is not 0 or NR(14)—is NR(16)R(17);

[2922] R(16) and R(17)

[2923] independently of one another are H, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms;

[2924] or

[2925] R(16) and R(17)

[2926] together are 4 or 5 methylene groups,

[2927]  of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chloro-phenyl);

[2928] and the other substituents R1, R3, R4, R5, R6, R7 and R8 in eachcase,

[2929] which are still not allocated by the definitions given above,

[2930] independently of one another are H, F, Cl, Br, I, CN, NO₂, CF₃,C₂F₅ or V_(p)Q_(q)U;

[2931] V is O, S, SO, SO₂, NR(60), OC═O, C═O, C(═O)NR(60), C(═O)O orCR(66)R(67);

[2932] R(60), R(66) and R(67)

[2933] independently of one another are H, alkyl having 1, 2, 3, 4, 5 or6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms orcycloalkyl having 3, 4, 5, 6 or 7 carbon atoms;

[2934] p is zero or 1;

[2935] Q is alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 CH₂ groups, whereone of these CH₂ groups can be replaced by O, S, NR(68) or o-, p- orm-phenylene;

[2936] R(68) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5 or 6 carbon atoms;

[2937] q is zero or 1;

[2938] U is H, alkyl having 1, 2, 3, 4, 5, 6 or 7 carbon atoms,cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms, C(═O)R(65), SO₂R(65),NR(61)R(62) or phenyl,

[2939] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, Br, CF₃, methyl, methoxyand NR(63)R(64);

[2940] R(63) and R(64)

[2941] independently of one another are H, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[2942] R(65) is N═C(NH₂)₂, NR(61)R(62) or OR(60);

[2943] R(61) and R(62)

[2944] independently of one another are H, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms;

[2945] or

[2946] R(61) and R(62)

[2947] together are 4 or 5 methylene groups,

[2948]  of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chlorophenyl);

[2949] or

[2950] U is an N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or9 carbon atoms,

[2951] where the N-containing heterocycle is linked via N or C and isnot substituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, Br, CF₃, methyl, methoxy and NR(63)R(64);

[2952] but where at least one of the substituents R5, R6, R7 and R8 isnot

[2953] hydrogen; and their pharmaceutically tolerable salts;

[2954] (96/F 141—EP-A 811610)

[2955] bb) ortho-substituted benzoylguanidines of the formula I

[2956] in which:

[2957] R(1) is H, F, Cl, Br, I, CN, NO₂, alkyl having 1, 2, 3, 4, 5, 6,7 or 8 carbon atoms, alkoxy having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkoxyhaving 3, 4, 5, 6, 7 or 8 carbon atoms or X_(a)—(CH₂)_(b)—(CF₂)_(b)—CF₃;

[2958] X is oxygen, sulfur or NR(9);

[2959] a is zero or 1;

[2960] b is zero, 1 or 2;

[2961] c is zero, 1, 2 or 3;

[2962] R(9) is H, alkyl having 1, 2, 3 or 4 carbon atoms or—C_(d)H_(2d)R(6);

[2963] d is zero, 1, 2, 3 or 4;

[2964] R(6) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms,phenyl, biphenylyl or naphthyl,

[2965]  where the aromatics phenyl, biphenylyl or naphthyl are notsubstituted or are substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(7)R(8);

[2966]  R(7) and R(8) are

[2967]  independently, H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2968] or

[2969] R(1) is —SR(10), —OR(10) or —CR(10)R(11)R(12);

[2970] R(10) is —C_(f)H_(2f)-cycloalkyl having 3, 4, 5, 6, 7 or 8 carbonatoms in the cycloalkyl ring, heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8or 9 carbon atoms or phenyl,

[2971] where heteroaryl and phenyl are unsubstituted or are substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;

[2972] f is zero, 1 or 2;

[2973] R(11) and (R12),

[2974] independently of each other, are defined as R(10) or are hydrogenor alkyl having 1, 2, 3 or 4 carbon atoms;

[2975] or

[2976] R(1) is phenyl, naphthyl, biphenylyi. or heteroaryl having 1, 2,3, 4, 5, 6, 7, 10 8, or 9 carbon atoms, the latter linked via a carbonor nitrogen atom of the ring,

[2977] each of which is unsubstituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino,

[2978] or

[2979] (R1) is —SR(13), —OR(13), —NHR(13), —NR(13)R(14), —CHR(13)R(15),—C[R(15)R(16)OH], —C≡CR(18), —C[R(19)]═CHR(18),—C[R(20)R(21)]_(k)—(CO)—[CR(22)R(23)]_(l)—R(24),

[2980] k is zero, 1, 2, 3 or 4;

[2981] l is zero, 1, 2, 3 or 4;

[2982] R(13) and R(14),

[2983] identically or differently, are—(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(kk)—R(17) or—(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(24);

[2984] R(17) is hydrogen or methyl,

[2985] g, h and i,

[2986]  identically or differently, are zero, 1, 2, 3 or 4;

[2987] kk is 1, 2, 3 or 4;

[2988] R(15) and R(16),

[2989] identically or differently, are hydrogen, alkyl having 1, 2, 3,4, 5 or 6 carbon atoms, or, together with the carbon atom carrying them,cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms;

[2990] R(18)

[2991] is phenyl,

[2992] which is unsubstituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(25)R(26);

[2993] R(25) and R(26) are

[2994]  H or alkyl having 1, 2, 3 or 4 carbon atoms;

[2995] or

[2996] R(18) is heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms,

[2997] which is unsubstituted or is substituted as phenyl;

[2998] or

[2999] R(18) is alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,

[3000] which is unsubstituted or is substituted by 1-3 OH;

[3001] or

[3002] R(18)

[3003] is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms;

[3004] R(19), R(20), R(21), R(22) and R(23),

[3005] identically or differently, are hydrogen or methyl;

[3006] R(24) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,cycloalkyl

[3007] having 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(m)H_(2m)—R(18);

[3008] m is 1, 2, 3 or 4;

[3009] one of the two substituents R(2) and R(3) is —O—CO—R(27);

[3010] R(27) is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, phenyl, biphenylyl,naphthyl, pyridyl or quinolinyl,

[3011] where phenyl, biphenylyl, naphthyl, pyridyl or quinolyl areunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(7)R(8);

[3012] R(7) and R(8)

[3013] independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms;

[3014] where one of the substituents R(2) and R(3)

[3015] is always defined as R(1);

[3016] R(4) and R(5)

[3017] independently of one another are hydrogen, alkyl having 1, 2, 3or 4 carbon atoms, alkoxy having 1, 2, 3 or 4 carbon atoms, F, Cl, Br,I, CN or —(CH₂)_(n)—(CF₂)_(o)—CF₃,

[3018] n is zeroor 1,

[3019] o is zero or 1,

[3020] and their pharmaceutically tolerable salts;

[3021] (96/F 154)

[3022] bc) benzoylguanidines of the formula I

[3023] in which:

[3024] R(1) is R(13)—SO_(m) or R (14)R(15)N—SO₂—;

[3025] m is 1 or 2;

[3026] R(13) is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, alkenylhaving 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(n)H_(2n)—R(16),

[3027] n is zero, 1, 2, 3 or 4;

[3028] R(16) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms,phenyl, biphenylyl or naphthyl,

[3029] where phenyl, biphenylyl and naphthyl are not substituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and

[3030] NR(25)R(26);

[3031] R(25) and R(26) are,

[3032]  independently of each other, hydrogen, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[3033] R(14) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkenyl having 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(n)H_(2n)—R(27),

[3034] n is zero, 1, 2, 3 or 4;

[3035] R(27) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms,phenyl, biphenylyl or naphthyl,

[3036] where phenyl, biphenylyl and naphthyl are not substituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(28)R(29);

[3037] R(28) and R(29) are,

[3038]  independently of each other, hydrogen, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[3039] R(15) is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms orperfluoroalkyl having 1, 2, 3 or 4 carbon atoms;

[3040] or

[3041] R(14) and R(15) are,

[3042] together, 4 or 5 methylene groups of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[3043] one of the substituents R(2) and R(3)

[3044] is hydrogen;

[3045] and the other of the substituents R(2) and R(3) in each case is—CHR(30)R(31);

[3046] R(30) is

[3047] —(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(r)—(CHOH)_(k)—R(32) or—(CH₂)_(g)—O-(CH₂-CH₂O )_(h)—R(24);

[3048] R(24) and R(32) are,

[3049] independently of each other, hydrogen or methyl;

[3050] g, h and i are,

[3051] identically or differently, zero, 1, 2, 3 or 4;

[3052] k is 1, 2, 3 or 4;

[3053] or the other of the substituents R(2) and R(3) in each case is

[3054] —C(OH)R(33)R(34);

[3055] R(31), R(33) and R(34) are,

[3056] identically or differently, hydrogen or alkyl having 1, 2, 3 or 4carbon atoms,

[3057] or

[3058] R(33) and R(34) are,

[3059] together, cycloalkyl having 3, 4, 5 or 6 carbon atoms;

[3060] or

[3061] R(33) is —CH₂OH;

[3062] R(4) is alkyl having 1, 2, 3 or 4 carbon atoms, alkoxy having 1,2, 3 or 4 carbon atoms, F, Cl, Br, I, CN or —(CH₂)_(n)—(CF₂)_(o)—CF₃;

[3063] n is zero or 1;

[3064] o is zero, 1 or 2;

[3065] and their pharmaceutically tolerable salts;

[3066] (96/F 202)

[3067] bd) indanylidineacetylguanidines of the formula I

[3068] in which:

[3069] R1, R2, R3, R4, R5 and R6

[3070] independently of one another are H, C₁-C₁₀-alkyl; haloalkylhaving 1-6 carbon atoms, O—C₁-C₁₀-alkyl, haloalkoxy having 1-6 carbonatoms, F, Cl, Br, I, aryl, substituted aryl, heteroaryl, substitutedheteroaryl, OH, O-lower alkyl, O-aryl, O-lower alkylaryl, O-substitutedaryl, O-lower alkyl-substituted aryl, O—C(═O)—C₁-C₄-alkylaryl,O—C(═O)—NH—C₁-C₄-alkyl, O—C(═O)—N(C₁-C₄-alkyl)₂, NO₂, CN, CF₃, NH₂,NH—C(═O)—C₁-C₄-alkyl, NH—C(═O)—NH₂, COOH, C(═O)—O—C₁-C₄-alkyl,C(═O)—NH₂, C(═O)—NH—C₁-C₄-alkyl, C(═O)—N(C₁-C₄-alkyl)₂, C₁-C₄—COOH,C₁-C₄-alkyl-C(═O)—O—C₁-C₄-alkyl, SO₃H, SO₂-alkyl; SO₂-alkylaryl,SO₂—N-(alkyl)₂, SO₂—N(alkyl)(alkylaryl), C(═O)—R11,C₁-C₁₀-alkyl-C(═O)-R11, C₂-C₁₀-alkenyl-C(═O)—R11,C₂-C₁₀-alkynyl-C(═O)—R11, NH—C(═O)—C₁-C₁₀-alkyl-C(═O)—R11 orO—C₁-C₁₁-alkyl-C(═O)-R11;

[3071] R11 is C₁-C₄-alkyl, C₁-C₄-alkynyl, aryl, substituted aryl, NH₂,NH—C₁-C₄-alkyl, N—(C₁-C₄-alkyl)₂, SO₃H, SO₂-alkyl, SO₂-alkylaryl,SO₂—N-(alkyl)₂ or SO₂—N(alkyl)(alkylaryl);

[3072] X is O, S or NH;

[3073] R7, R8, R9 and R10

[3074] independently of one another are H, alkyl, cycloalkyl, aryl,alkylaryl,

[3075] or

[3076] R8 and R9

[3077] together are part of a 5-, 6- or 7-membered heterocyclic ring;

[3078] or their pharmaceutically acceptable salts;

[3079] (96/F 226)

[3080] be) phenyl-substituted alkenylcarboxylic acid guanidides of theformula

[3081] in which:

[3082] T is

[3083] R(A) is hydrogen, F, Cl, Br, I, CN, OH, OR(6), (C₁-C₄)-alkyl,O_(r)(CH₂)_(a)C_(b)F_(2b+1), (C₃-C₈)-cycloalkyl oder NR(7)R(8)

[3084] r is zero or 1;

[3085] a is zero, 1, 2, 3 or 4;

[3086] b is 1, 2, 3 or 4;

[3087] R(6) is (C₁-C₄)-alkyl, (C₁-C₄)-perfluoroalkyl, (C₃-C₆)-alkenyl,(C₃-C₈)-cycloalkyl, phenyl or benzyl,

[3088] the phenyl nucleus not being substituted or being substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(9)R(10),

[3089] R(9) and R(10)

[3090]  are H, (C₁-C₄)-alkyl or (C₁-C₉)-perfluoroalkyl;

[3091] R(7) and R(8)

[3092]  independently of one another are defined as R(6);

[3093] or

[3094] R(7) and R(8)

[3095]  together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;

[3096] R(B), R(C) and R(D)

[3097] independently are defined as R(A);

[3098] x is zero, 1 or 2;

[3099] y is zero, 1 or 2;

[3100] R(F) is hydrogen, F, Cl, Br, I, CN, OR(12), (C₁-C₈)-alkyl,O_(p)(CH₂)_(f)C_(g)F_(2g+1), (C₃-C₈)-cycloalkyl or (C₁-C₉)-heteroaryl;

[3101] p is zero or 1;

[3102] f is zero, 1, 2, 3 or 4;

[3103] g is 1, 2, 3, 4, 5, 6, 7 or 8;

[3104] R(12) is (C₁-C₈)-alkyl, (C₁-C₄)-perfluoroalkyl, (C₃-C₈)-alkenyl,(C₃-C₈)-cycloalkyl, phenyl or benzyl,

[3105] the phenyl nucleus not being substituted or being substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(13)R(14);

[3106] R(13) and R(14)

[3107]  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[3108] R(E) is defined independently as R(F);

[3109] R(1) is defined independently as T;

[3110] or

[3111] R(1) is hydrogen, —O_(k)C_(m)H_(2m+1),—O_(n)(CH₂)_(p)C_(q)F_(2q+1), F, Cl, Br, I, CN, —(C═O)—N═C(NH₂)₂,—SO_(r)R(17), —SO_(r2)NR(31)R(32), —O_(u)(CH₂)_(v)C₆H₅,—O_(u2)—(C₁-C₉)-heteroaryl or —S_(u2)—(C₁-C₉)-heteroaryl;

[3112] k is zero or 1;

[3113] m is zero,1, 2, 3, 4, 5, 6, 7 or 8;

[3114] n is zero or 1;

[3115] p is zero, 1, 2, 3 or 4;

[3116] q is 1, 2, 3, 4, 5, 6, 7 or 8;

[3117] r is zero, 1 or 2;

[3118] r2 is zero, 1 or 2;

[3119] R(31) and R(32)

[3120] independently of one another are hydrogen, (C₁-C₈)-alkyl or(C₁-C₈)-perfluoroalkyl;

[3121] or

[3122] R(31) and R(32)

[3123] are, together, 4 or 5 methylene groups of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

[3124] R(17) is (C₁-C₈)-alkyl;

[3125] u is zero or 1;

[3126] u2 is zero or 1;

[3127] v is zero, 1, 2, 3 or 4;

[3128] where the phenyl nucleus is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy, —(CH₂)_(w)NR(21)R(22), NR(18)R(19) and(C₁-C₉)-heteroaryl;

[3129] R(18), R(19), R(21) and R(22)

[3130] independently of one another are (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl;

[3131] w is 1, 2, 3 or 4;

[3132] where the heterocycle of the (C₁-C₉)-heteroaryl is unsubstitutedor substituted by 1-3 substituents selected from the group consisting ofF, Cl, CF₃, m-ethyl or methoxy;

[3133] R(2), R(3), R(4) and R(5)

[3134] independently of one another are defined as R(1),

[3135] or

[3136] R(1) and R(2) or R(2) and R(3)

[3137] in each case together are —CH—CH═CH—CH—,

[3138] which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy,—(CH₂)_(w2)NR(24)R(25) and NR(26)R(27);

[3139] R(24), R(25), R(26) and R(27)

[3140] are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;

[3141]  w2 is 1, 2, 3 or 4;

[3142] the radical T being present in the molecule at least twice, butonly three times at most;

[3143] and their pharmaceutically tolerable salts;

[3144] (97/F 082)

[3145] bf) benzoylguanidines of the formula I

[3146] in which:

[3147] R(1) is CF₃;

[3148] one of the substituents R(2) and R(3)

[3149] is hydrogen;

[3150] and the other substituent R(2) or R(3) in each case

[3151] is —C(OH)(CH₃)—CH₂OH, —CH(CH₃)—CH₂OH or —C(OH)(CH₃)₂;

[3152] R(4) is methyl, methoxy, Cl or CF₃;

[3153] and their pharmaceutically tolerable salts.

[3154] (DE 195 02 895, DE 44 30212, EP 667 341, DE 44 04 183, EP 708088, EP 723 963, EP 0 694 537, DE 44 21 495, EP 699 660, EP 699 663, EP699 666, DE4337611, EP 0719766, WO94/26709, WO 9604 241, EP 726 254,U.S. Pat. No. 4,251,545, DE 35-02 629, WO 84/00875, Kumamoto et al.,Pharm. Bull. [1966], 7-13; U.S. Pat. No. 3,780,027, JP 8225513; EP 743301)

[3155] II. Also Suitable are Compounds of the Formula

[3156] in which:

[3157] W, Y and Z

[3158] are a nitrogen atom or a carbon atom substituted by R(2) or R(3)or R(4);

[3159] R(1) is hydrogen, A, Hal, —CF₃, —CH₂F, —CHF₂, —CH₂CF₃, —C₂F₅,—CN, —NO₂, -ethynyl, or an X—R′;

[3160] A is alkyl having I to 6 carbon atoms;

[3161] Hal is F, Cl, Br or I;

[3162] X is oxygen, S or NR″;

[3163] R″ is hydrogen, A or a cyclic methylene chain having 3 to 7carbon atoms;

[3164] R′ is H, A, HO—A—, HOOC—A—, (C₃-C₇)-cycloalkyl,(C₆-C₈)-cycloalkylalkyl, CF₃, CH₂F, CHF₂, CH₂—CF₃, Ph, —CH₂—Ph or Het;

[3165] Ph is phenyl, naphthyl or biphenylyl which is unsubstituted ormono-, di- or trisubstituted by A, OA, NR′R″, Hal, CF₃;

[3166] Het is a mono- or binuclear saturated, unsaturated or aromaticheterocycle having 1 to 4 nitrogen, oxygen and/or sulfur atoms,

[3167] which is unsubstituted or mono-, di- or trisubstituted by Hal,CF₃, A, OH, OA, —X—R′, —CN, —NO₂, and/or carbonyl oxygen,

[3168] where Het is bonded via N or an alkylene chain C_(m)H_(2m) wherem=zero to 6;

[3169] or

[3170] R′ and R′″

[3171] together are alkylene having 4-5 carbon atoms, in which one CH₂group can also be replaced by oxygen, S, NH, N—A, N—Ph and N—CH₂—Ph;

[3172] R(2) and R(3)

[3173] independently of one another are hydrogen, Hal, A, HO—A—, X—R′,—C(═N—OH)—A, A—O—CO—(C₁-C₄)-alkyl-, CN, NO₂, COOH, halogen-substitutedA, in particular CF₃, CH₂F, CHF₂, C₂F₅, CH₂CF₃, or S(O)_(n)R′″;

[3174] R′″ is A, Ph or -Het;

[3175] n is zero, 1 or 2;

[3176] or

[3177] R(2) and R(3)

[3178] independently of one another are SO₂NR′R″, Ph or —O—Ph,—O—CH₂—Ph, —CO—A, —CHO, —COOA, —CSNR′R″, CONR′R″, —CH═CH—COOH,—CH═CH—COOA, indenyl, indanyl, decahydronaphthyl, cyclopentenyl,dihydrothienyl, dihydrofuryl, heterobicyclyl, alkylthienyl, halothienyl,haloalkylthienyl, acylthienyl, halofuryl, haloalkylfuryl or pyrrolyl;

[3179] or

[3180] R(2) and R(3)

[3181] independently of one another are R(5)—O—;

[3182] R(5) is hydrogen, A, (C₁-C₆)-alkenyl or (C₃-C₇)-cycloalkyl;

[3183] R(4) is Ph, Het, —O-Het; CF₃, S(O)_(n)R′″, —SO₂NR′R″, alk;

[3184]  or

[3185] two of the substituents R(1) to R(4)

[3186] together are a group —O—CR(6)R(7)—CO—NR(8)—,

[3187] where R(2) has the meaning indicated;

[3188] R(6), R(7), R(8) and R(9)

[3189]  independently of one another are H or A;

[3190] or

[3191] R(8) is (C₅-C₇)-cycloalkyl;

[3192] or

[3193] R(9) is cyano;

[3194] alk is straight-chain or branched (C₁-C₈)-alkyl or(C₃-C₈)-cycloalkyl, which is unsubstituted or mono-, di- ortrisubstituted by A;

[3195] or

[3196] alk is an ethenyl or ethynyl radical which is substituted by H,A, Ph or Het.

[3197] (DE 4127 026, DE 43 37 609, JP 07025768, Edward J. Cragoe, Jr.,DIURETICS [Chemistry, Pharmacology and Medicine), J. Wiley & Sons(1983), 303-341]

[3198] III. Compounds of the Formula

[3199] in which:

[3200] X is H, Hal, (Hal)₃C—, (C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl,substituted phenyl, (C₁-C₅)-alkyl-S— or (C₁-C₅)-alkyl-SO₂—;

[3201] Y is NH₂ or substituted amino;

[3202] or

[3203] X and Z

[3204] together are a —(CH₂)₄— or a 1,3-butadienylene chain;

[3205] or

[3206] Z is H, Hal, OH, HS, (C₁-C₅)-alkyl, (C₃-C₆)-cycloalkyl,substituted phenyl;

[3207] or

[3208] Z is an amino group —NR(1)R(2);

[3209] R(1) is H, straight- and branched-chain, optionally substituted(C₁-C₈)-alkyl,

[3210] which can be interrupted by oxygen;

[3211] or

[3212] R(1) is (C₃-C₈)-alkenyl, (C₃-C₈)-alkynyl, (C₃-C₇)-cycloalkyl orOH-substituted phenyl or OH-substituted phenyl-(C₁-C₄)-alkyl orOH-substituted (C₃-C₇)-cycloalkyl;

[3213] R(2) is 1-morpholino, hydrogen or a straight or branched(C₁-C₈)-alkyl chain,

[3214] which can be interrupted by oxygen or an amino group,

[3215] which straight or branched (C₁-C₈)-alkyl chain is unsubstitutedor substituted by

[3216] a substituted or unsubstituted mono- or polynuclear heterocyclewhich contains nitrogen, oxygen or sulfur atoms;

[3217] or

[3218] which alkyl chain is substituted by phenyl,

[3219] optionally mono- or polysubstituted by (C₁-C₄) alkoxy, optionallysubstituted by OH, alkylamino, alkyl or phenyl;

[3220] or

[3221] by an aminocarbonyl group

[3222] or

[3223] by hydroxyl or (C₁-C₄)-alkoxy groups,

[3224] or

[3225] R(2) is phenyl,

[3226] unsubstituted or substituted by alkyl, alkoxy, an amino group,which as substituents carries:

[3227] H, a mono- or polynuclear heterocycle which contains nitrogen,oxygen or sulfur atoms, which is unsubstituted or substituted by H, Halor (C₁-C₄)-alkyl;

[3228] a phenyl radical,

[3229]  unsubstituted or substituted by a substituent selected from thegroup consisting of (C₁-C₄)-alkyl, (C₁-C₄)-alkoxy, Hal and OH;

[3230] or

[3231] R(2) is 1-piperidino,

[3232] unsubstituted or substituted in the 4-position by an acyl radicalof an aliphatic, alicyclic, aromatic or heteroaromatic carboxylic acid,(C₁-C₈) alkyl, which for its part can be substituted by OH or(C₁-C₄)-alkoxy or a (C₁-C₄)-alkoxy-substituted phenyl radical;

[3233] or

[3234] R(2) is amidino,

[3235] which is unsubstituted or substituted by phenyl,

[3236] which is unsubstituted or substituted by Hal or alkyl;

[3237] or

[3238] R(2) is an acyl radical of an aliphatic, alicyclic, aromatic orheteroaromatic carboxylic acid,

[3239] or

[3240] R(2) is a (C₁-C₈) alkyl chain, which can be substituted by aphenyl radical carrying OH, alkoxy or alkyl radicals.

[3241] or

[3242] R(1) and R(2)

[3243] together with the nitrogen atom to which they are bonded, are apiperazine ring,

[3244] which is unsubstituted or, via a (C₁-C₆)-methylene chain, carriesa mono- or polynuclear heterocycle,

[3245]  which contains nitrogen, oxygen or sulfur (DE 4127 026 and DE 4337 609).

[3246] Hal is F, Cl, Br or I.

[3247] (EP 708 091, EP 622 356, JP 5-125085)

[3248] IV. Likewise suitable are indoloylguanidine derivatives of theformula

[3249] in which

[3250] R(2) is hydrogen, unsubstituted or substituted (C₁-C₈)-alkyl,(C₃-C₇)-cycloalkyl, OH, (C₁-C₆)-alkyl-O—, an aromatic radical or a group—CH₂—R(20);

[3251] R(20) is (C₂-C₆)-alkenyl or (C₂-C₆)-alkynyl;

[3252] R(1) is 1 to 5 identical or different substituents, which are:

[3253] hydrogen, unsubstituted or substituted (C₁-C₈)-alkyl,(C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl, (C₃-C₇)-cycloalkyl, halogen, —NO₂,(C₂-C₈)-alkanoyl, arylalkanoyl having up to 10 carbon atoms, aroylhaving up to 11 carbon atoms, —COOH, (C₂-C₆)-alkoxycarbonyl, an aromaticgroup or one of the following mentioned groups: —OR(3), —NR(6)R(7) or—S(O)nR(40);

[3254] R(3) is hydrogen, (C₁-C₈)-alkyl, substituted (C₁-C₈)-alkyl,(C₃-C₇)-cycloalkyl, an aromatic radical or a group —CH₂-R(30); R(30) isalkenyl or alkynyl;

[3255] R(6) and R(7)

[3256] independently of one another are hydrogen, unsubstituted orsubstituted (C₁-C₈)-alkyl, (C₃-C₇)-cycloalkyl, (C₂-C₈)-alkanoyl, anarylalkanoyl group having up to 10 carbon atoms, an aroyl group havingup to 11 carbon atoms, an aromatic group or —CH₂—R(60);

[3257] R(60) is (C₂-C₆)-alkenyl or (C₂-C₆)-alkynyl;

[3258] or

[3259] R(6) and R(7)

[3260] together with the nitrogen atom are a 5-7-membered cyclic amine,which can additionally contain further heteroatoms in the ring;

[3261] n is zero, 1 or 2;

[3262] R(40) is unsubstituted or substituted (C₁-C₈)-alkyl, or anaromatic group, or a group

[3263] A is oxygen , —S(O)_(n)— or —N(R50)—;

[3264] R(50) is hydrogen or (C₁-C₈)-alkyl;

[3265] R′ is hydrogen, unsubstituted or substituted (C₁-C₈)-alkyl, inwhich the ring represents a saturated 3-8-membered heterocycle having anitrogen atom,

[3266] said substituted alkyl carries one or more groups selected fromthe group consisting of halogen, —OH, (C₁-C₆)-alkoxy, —CN, —COOH,(C₂-C₆)-alkoxycarbonyl, (C₂-C₈)-alkanoyl, arylalkanoyl having up to 10carbon atoms, aroyl having up to 11 carbon atoms, an aromatic group,—CONR(4)(R5),

[3267] R(4) and R(5)

[3268] identically or differently are hydrogen or (C₁-C₈)-alkyl;

[3269] or

[3270] R(4) and R(5)

[3271] are connected to one another and together form a 5-7-memberedcyclic amine which can additionally contain further heteroatoms in thering,

[3272] or said substituted alkyl carries a group

[3273] in which:

[3274] E is a nitrogen atom or a CH group;

[3275] R″ is hydrogen, (C₁-C₈)-alkyl which is unsubstituted or

[3276] substituted by OH or substituted (C₁-C₈)-alkyl, (C₁-C₆)-alkoxy,—CN, —COOH, (C₂-C₆)-alkoxycarbonyl, (C₂-C₈)-alkanoyl, aralkanoyl havingup to 10 carbon atoms, aroyl having up to 11 carbon atoms, an aromaticgroup, —NR(6)R(7), —CONR(4)R(5);

[3277] R(4) and R(5)

[3278]  independently of one another are hydrogen or (C₁-C₈)-alkyl;

[3279]  where the cyclic system of the formula

[3280]  is a 3-8-membered saturated aliphatic or heterocyclic ringsystem having a nitrogen atom,

[3281] and where the aromatic groups mentioned are an aryl radicalhaving up to 10 carbon atoms, a 5- or 6-membered heteroaryl radicalhaving 1-4 nitrogen atoms, a 5- or 6-membered heteroaryl groupcontaining 1 or 2 nitrogen atoms and a heteroatom which is oxygen orsulfur, or furyl, and where the aryl radicals mentioned can beunsubstituted or substituted by unsubstituted (C₁-C₈)-alkyl orsubstituted (C₁-C₈)-alkyl, halogen, —NO₂, (C₂-C₆)-alkoxycarbonyl, COOH,—OR(3), NR(6)R(7), —CONR(4)R(5), —SO₂NR(6)R(7) or S(O)_(n)R(40),

[3282] where R(1) and the guanidinocarbonyl radical can be in anydesired position of the 5- or 6-membered ring of the indole system, andthe appropriate pharmaceutically tolerable salts.

[3283] (WO 95 04052)

[3284] V. Additionally suitable are heterocyclic guanidine derivativesof the formula

[3285] in which:

[3286] X is —O—, —S—, —NH—, —N[(C₁-C₄)-alkyl]- or —N(phenyl)—;

[3287] R(1), R(2) and R(3)

[3288] are hydrogen, halogen, (C₁-C₄)-alkyl, (C₁-C₄)-alkyl-O—, phenyl,benzyl;

[3289] or

[3290] two of the substituents R(1), R(2) and R(3)

[3291] together with one side of the benzo system are a 4-6-memberedcarbocyclic ring;

[3292] R(4) and R(5)

[3293] independently of one another are hydrogen, (C₁-C₁₂)-alkyl,benzhydryl, aralkyl,

[3294] which is unsubstituted or substituted by one or more substituentsfrom the groups halogen, (C₁-C₄)-alkyl, (C₁-C₄)-alkyl-O— or —CF₃,—(CH₂)_(m)—CH₂—T,

[3295] m is zero to 3;

[3296] T is —CO—O—T(1);

[3297] T(1) is hydrogen or (C₁-C₄)-alkyl;

[3298] Cy is a benzo-fused unsaturated or dihydro-5-membered ringheterocycle

[3299]  a pyrazole or imidazole ring of the formula

[3300]  a naphthyl radical or a dihydro- or tetrahydronaphthyl radical

[3301]  a 2-, 3- or 4-pyridyl radical

[3302] z is N— or CH; a thienyl radical

[3303] R(6) is hydrogen, halogen, hydroxyl, (C₁-C₁₀)-alkyl,(C₁-C₁₀)-alkyl-O—, phenoxy, (C₁-C₁₀)-alkyloxymethyloxy- or—(O)_(n)S—R(9);

[3304] n is zero, 1 or 2;

[3305] R(9) is (C₁-C₁₀)-alkyl, thienyl, pyridyl, thiazolyl,thiadiazolyl, imidazolyl, pyrazolyl or phenyl,

[3306] each of which is unsubstituted or mono- or disubstituted byhalogen, (C₁-C₄)-alkyl or (C₁-C₄)-alkyl-O—;

[3307] R(7) and R(8)

[3308] are hydrogen, halogen, hydroxyl, (C₁-C₁₀)-alkyl,(C₁-C₁₀)-alkyl-O—, phenyl, phenoxy or (C₁-C₁₀)-alkoxymethyloxy;

[3309] or

[3310] Cy is phenyl,

[3311] which is unsubstituted or is mono- or disubstituted by halogen,(C₁-C₄)-alkyl or (C₁-C₄)-alkyl-O—;

[3312] or

[3313] Cy is —Gr—Am;

[3314] Gr is —R(13)—R(12)—(CH₂)_(q)—C[W][W(1)]—(CH₂)_(q)—; R(13)R(14)—or —R(15)—;

[3315] R(12) is a single bond, —O—, —(O)_(n)S—, —CO— or —CONH—;

[3316] n is zero, 1 or 2;

[3317] R(13) is a single bond, phenyl, thienyl, pyridyl, thiazolyl,thiadiazolyl, imidazolyl or pyrazolyl;

[3318] R(14) is a single bond or SO₂—;

[3319] R(15) is (C₂-C₁₀)-alkenyl or (C₂-C₁₀)-alkynyl;

[3320] W and W(1)

[3321] independently of one another are hydrogen, (C₁-C₄)-alkyl;

[3322] or

[3323] W and W(1)

[3324] cyclically connected to one another are a (C₃-C₈)-hydrocarbonring;

[3325] q and q′

[3326] are zero to 9;

[3327] Am is —NR(10)R(11);

[3328] R(10) is hydrogen, (C₁-C₄)-alkyl or benzyl,

[3329] R(11) is (C₁-C₄)-alkyl, phenyl or benzyl;

[3330] or

[3331] R(10) and R(11)

[3332] together are a (C₃-C₁₀)-alkylene group,

[3333]  which is unsubstituted or substituted by —COOH,(C₁-C₅)-alkoxycarbonyl, (C₂-C₄)-hydroxylalkylene or benzyl;

[3334] or

[3335] Am is pyrrolyl, pyridyl, pyrazolyl, morpholinyl, dihydropyridyl,tetrahydropyridyl, quinuclidinyl, imidazolyl, 3-azabicyclo[3.2.1]octyl,

[3336] which is unsubstituted or substituted by (C₁-C₄)-alkyl,

[3337] or

[3338] Am is azabicyclo[3.2.2]nonyl;

[3339] or

[3340] Am is a piperazine group of the formula

[3341] R(16) is hydrogen, (C₁-C₄)-alkyl, (C₃-C₆)-cycloalkyl, phenyl,tolyl, methoxyphenyl, halophenyl, diphenylmethylene, benzyl or pyridyl;

[3342] or

[3343] Am is an azido group —(O)_(t)—(CH₂)_(q)—C[W][W(1)]—(CH₂)_(q)′—N₃;

[3344] t is zero or 1;

[3345] where W and W(1) have the previously indicated meaning;

[3346] and the optical enantiomers and the pharmacologically tolerablesalts.

[3347] VI. Additionally suitable are the guanidine compounds such as aredescribed in EP-743 301 (DE 195 17 848), EP 758 644 (DE 195 29 612), EP760 365 (DE 195 31138)

[3348] where R1=R2 is H, halo, alkyl, CN, NO₂, perfluoroalkyl,SO_(n)CF₃; R3 is CH═CH₂, CH₂—CH=CH₂, CH₂—CH₂—CH═CH₂, cycloalkenyl,cycloalkenylalkyl;

[3349] n is zero, 1 or 2;

[3350] R4 is alkyl, (substituted) phenyl,

[3351] or as described in DE 195 48 708, WO 97 25 310, WO 97 27 183, DE196 01303, EP 787 728, JP 82 25 513, JP 090 59 245, JP 090 67 332, JP090 67 340, WO 97 11055 and EP 743 301.

[3352] The disclosures of all the documents cited in this applicationare specifically incorporated by reference herein. The disclosures ofGerman Priority Applications Nos. 19742096.6 (Sep. 24, 1997) and19750498.1 (Nov. 14, 1997) are also specifically incorporated byreference herein.

What is claimed is:
 1. A method for the treatment or prophylaxis of adisturbance of the central nervous system which comprises administeringto a host in need of such treatment or prophylaxis an effective amountof an inhibitor of the Na⁺/H⁺ exchanger.
 2. A method as claimed in claim1, wherein the inhibitor of the Na⁺/H⁺ exchanger is: a) abenzoylguanidine of the formula

in which: R(1) or R(2) is R(6)—S(O)_(n)— or R(7)R(8)N—O₂S—; and theother substituent R(1) or R(2) in each case is H, F, Cl, Br,(C₁-C₄)-alkyl, (C₁-C₄)-alkoxy or phenoxy, which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting offluorine, chlorine, methyl and methoxy; or the other substituent R(1) orR(2) in each case is R(6)—S(O)_(n) or R(7)R(8)N—; n is zero, 1 or 2;R(6) is (C₁-C₆)-alkyl, (C₅-C₇)-cycloalkyl, cyclopentylmethyl,cyclohexylmethyl or phenyl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of fluorine, chlorine,methyl and methoxy; R(7) and R(8) identically or differently are H or(C₁-C₆)-alkyl; or R(7) is phenyl-(CH₂)_(m); m is 1-4; or R(7) is phenyl,which is unsubstituted or substituted by 1-2 substituents selected fromthe group consisting of fluorine, chlorine, methyl and methoxy; or R(7)and R(8) together are a straight-chain or branched (C₄-C₇)-chain, wherethe chain can additionally be interrupted by O, S or NR(9); R(9) is H ormethyl; or R(7) and R(8) together with the nitrogen atom to which theyare bonded, are a dihydroindole, tetrahydroquinoline ortetrahydroisoquinoline system; R(3), R(4) and R(5) independently of oneanother are H or (C₁-C₂)-alkyl, or R(3) and R(4) together are a(C₂-C₄)-alkylene chain; or R(4) and R(5) together are a (C₄-C₇)-alkylenechain; or a pharmaceutically tolerable salt thereof; b) abenzoylguanidine of the formula

in which: R(1) is R(4)—SO_(m) or R(5)R(6)N—SO₂—; m is zero, 1 or 2; R(4)and R(5) are C₁-C₈-alkyl, C₃-C₆-alkenyl or —C_(n)H_(2n)—R(7); n is zero,1, 2, 3 or 4; R(7) is C₅-C₇-cycloalkyl or phenyl, which is unsubstitutedor substituted by 1-3 substituents selected from the group consisting ofF, Cl, CF₃, methyl, methoxy and NR(8)R(9); R(8) and R(9)  are H orC₁-C₄-alkyl; or R(5) is H; R(6) is H or C₁-C₄-alkyl, or R(5) and R(6)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by an O, S, NH, N—CH₃ or N-benzyl; R(2) is hydrogen, F, Cl, Br,(C₁-C₄)-alkyl-, O—(CH₂)_(m)C_(p)F_(2p+1) or —X—R(10); m is zero or 1; pis 1, 2 or 3; X is O, S or NR(11); R(10) is H, C₁-C₆-alkyl,C₅-C₇-cycloalkyl, cyclohexylmethyl, cyclopentylmethyl or—C_(n)H_(2n)—R(12); n is zero, 1, 2, 3 or 4; R(12) is phenyl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(8)R(9); R(8) and R(9)are H or C₁-C₄-alkyl; R(11) is hydrogen or C₁-C₃-alkyl; or R(10) andR(11) together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by O, S, NH, N—CH₃ or N-benzyl; R(3) is defined as R(1), oris C₁-C₆-alkyl, nitro, cyano, trifluoromethyl, F, Cl, Br, I or —X—R(10);X is O, S or NR(11); R(10) is H, C₁-C₆-alkyl, C₅-C₇-cycloalkyl,cyclohexylmethyl, cyclopentylmethyl or —C_(n)H_(2n)—R(12); n is zero to4; R(12) is phenyl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy und NR(8)R(9); R(8) and R(9)  are H or C₁-C₄-alkyl; R(11) isC₁-C₃-alkyl, or R(10) and R(11) together are 4 or 5 methylene groups, ofwhich one CH₂ group can be replaced by O, S, NH, N—CH₃ or N-benzyl; or apharmaceutically tolerable salt thereof; c) an ortho-substitutedbenzoylguanidine of the formula

in which: R(1) is F, Cl, Br, I, C₁-C₆-alkyl or —X—R(6); X is O, S, NR(7)or Y—ZO; Y is O or NR(7); Z is C or SO; R(6) is H, C₁-C₆-alkyl,C₅-C₇-cycloalkyl, cyclohexylmethyl, cyclopentylmethyl,—(CH₂)_(m)C_(p)F_(2p+1) or —C_(n)H_(2n)—R(8); m is zero or 1; p is 1-3;n is zero to 4; R(8) is phenyl, which is unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(9)R(10); R(9) and R(10)  are H or C₁-C₄-alkyl;R(7) is H or C₁-C₃-alkyl; or R(6) and R(7) together are 4 or 5 methylenegroups, of which one CH₂ group can be replaced by O, S, NH, N—CH₃ orN-benzyl; R(3) is H or —X—R(6); X is O, S, NR(7) or Y—ZO; R(7) is H orC₁-C₃-alkyl; Y is O or NR(7); where Y is bonded to the phenyl radical ofthe formula I, Z is C or SO; R(6) is H, C₁-C₆-alkyl, C₅-C₇-cycloalkyl,cyclohexylmethyl, cyclopentylmethyl, —(CH₂)_(m)C_(p)F_(2p+1) or—C_(n)H_(2n)—R(8); m is zero or 1; p is 1-3; n is zero to 4; R(8) isphenyl, which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10); R(9) and R(10)  are H or C₁-C₄-alkyl; or R(6) and R(7)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by O, S, NH, N—CH₃ or N-benzyl; R(2) and R(4) identically ordifferently are R(11)—SO_(q)— or R(12)R(13)N—SO₂—; q is zero -2; R(11)is C₁-C₄-alkyl, which is unsubstituted or carries phenyl as asubstituent, where phenyl is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(9)R(10); R(9) and R(10) are H or C₁-C₄-alkyl; R(12) andR(13) are defined as R(6) and R(7); or one of the two radicals R(2) orR(4) is hydrogen or is defined as R(1); R(5) is H, methyl, F, Cl ormethoxy, or a pharmaceutically tolerable salt thereof; d) abenzoylguanidine of the formula

in which: R(1) or R(2) is an amino group —NR(3)R(4); R(3) and R(4)identically or differently are H, C₁-C₆-alkyl or C₃-C₇-cycloalkyl; orR(3) is phenyl-(CH₂)_(p)—; p is 0, 1, 2, 3 or 4; or R(3) is phenyl,where the phenyl in each case is unsubstituted or carries one to twosubstituents selected from the group consisting of fluorine, chlorine,methyl and methoxy; or R(3) and R(4) together can be a straight-chain orbranched C₄-C₇-methylene chain, where one —CH₂— member of the methylenechain can be replaced by oxygen, S or NR(5); R(5) is H or lower alkyl;the other substituent R(1) or R(2) in each case is H, F, Cl,C₁-C₄-alkyl, C₁-C₄-alkoxy, CF₃, C_(m)F_(2m+1)—CH₂—, benzyl or phenoxy,where the respective phenyl radical is unsubstituted or carries one totwo substituents selected from the group consisting of methyl, methoxy,fluorine and chlorine; m is 1, 2 or 3; or a pharmaceutically tolerablesalt thereof; e) a benzoylguanidine of the formula

in which: R(1) is R(4)—SO_(m) or R(5)R(6)N—SO₂—; m is zero, 1 or 2; R(4)and R(5) are C₁-C₈-alkyl, C₃-C₆-alkenyl or —C_(n)H_(2n)—R(7); n iszero,1, 2, 3 or 4; R(7) is C₅-C₇-cycloalkyl or phenyl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(8)R(9); R(8) and R(9) are H or C₁-C₁-alkyl; or R(5) is H; R(6) is H or C₁-C₄-alkyl; or R(5)and R(6) together are 4 or 5 methylene groups, of which one CH₂ groupcan be replaced by an O, S, NH, N—CH₃ or N-benzyl; R(2) is hydrogen,straight-chain or branched (C₅-C₈)-alkyl, —CR(13)═CHR(12) or —C≡CR(12);R(12) is phenyl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(14)R(15); R(14) and R(15) are H or (C₁-C₄)-alkyl; orR(12) is (C₁-C₉)-heteroaryl, which is unsubstituted or substituted asphenyl, or R(12) is (C₁-C₆)-alkyl, which is unsubstituted or substitutedby 1-3 OH, or R(12) is (C₃-C₈)-cycloalkyl; R(13) is hydrogen or methyl,or R(12) is (C₃-C₈)-cycloalkyl, (C₃-C₈)-cycloalkyl-(C₁-C₄)-alkyl,phenyl, C₆H₅—(C₁-C₄)-alkyl, naphthyl, biphenylyl,1,1-diphenyl-(C₁-C₄)-alkyl, cyclopentadienyl, pyridyl, pyrrolyl,furanyl, thienyl, thiazolyl, oxazolyl, indenyl, quinolyl, indolyl,benzofuranyl, benzothienyl, benzothiazolyl, benzoxazolyl, imidazolyl,pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, pyrazinyl,pyrimidinyl, pyridazinyl, indazolyl, isoquinolyl, phthalazinyl,quinoxalinyl, quinazolinyl or cinnolinyl; R(3) is defined as R(2); andwhere the aromatic substituents R(2) and R(3) are unsubstituted orsubstituted by 1-3 substituents selected from F, Cl, CF₃, (C₁-C₄)-alkyland -alkoxy, and NR(10)R(11) with R(10) and R(11) being H or(C₁-C₄)-alkyl; or a pharmaceutically tolerable salt thereof; f) abenzoylguanidine of the formula

in which: R(1) or R(2) is R(3)—S(O)_(n)— or R(4)R(5)N—SO₂—; the othersubstituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I,C₁-C₄-alkyl, C₁-C₄-alkoxy, benzyloxy or phenoxy, which is unsubstitutedor carries one to three substituents selected from the group consistingof fluorine, chlorine, methyl, methoxy, hydroxyl and benzyloxy,R(3)—S(O)_(n), —NR(4)R(5) or 3,4-dehydropiperidine; R(3) is C₁-C₆-alkyl,C₅-C₇-cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, whichis unsubstituted or carries one to three substituents selected from thegroup consisting of fluorine, chlorine, methyl and methoxy; R(4) andR(5) identically or differently, are H or C₁-C₆-alkyl; or R(4) isphenyl-(CH₂)_(m)—; m is 1, 2, 3 or 4; or R(4) is phenyl, which isunsubstituted or carries one to two substituents selected from the groupconsisting of fluorine, chlorine, methyl and methoxy; or R(4) and R(5)together are a straight-chain or branched C₄-C₇-chain, where the chaincan additionally be interrupted by O, S or NR(6), R(6) is H or methyl;or R(4) and R(5) together with the nitrogen atom to which they arebonded, are a dihydroindole, tetrahydroquinoline ortetrahydroisoquinoline system; n is zero, 1 or 2; or a pharmaceuticallytolerable salt thereof; g) an isoquinoline of the formula

in which: R(1) is hydrogen, alkyl, cycloalkyl, arylalkyl, alkenyl,substituted aminoalkyl or an aryl or heteroaryl ring; where the ringsare unsubstituted or substituted by 1-3 substituents selected from thegroup consisting of halogen, nitro, amino, mono(lower alkyl)amino,di(lower alkyl)amino, lower alkyl, lower alkoxy, benzyloxy, phenoxy,hydroxyl, and trifluoromethyl, R(2) is hydrogen, halogen, alkyl or aryl;which is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of halogen, nitro, amino, mono(lower alkyl)amino,di(lower alkyl)amino, lower alkyl, lower alkoxy, benzyloxy, phenoxy, andhydroxyl, G is —N═C{[NR(3)R(4)][N(R5)R(6)]}; R(3), R(4), R(5) and R(6)are hydrogen, X(2), X(3) and X(4) independently of one another arehydrogen, halogen, nitro, amino, alkyl, sulfonamide, mono(loweralkyl)amino, di(lower alkyl)amino, lower alkyl, benzyloxy, hydroxyl;X(1) is hydrogen, oxygen, sulfur or NR(7); R(7) is hydrogen, alkyl,cycloalkyl, arylalkyl, alkenyl, substituted aminoalkyl or an aryl or aheteroaryl ring; which rings are unsubstituted or substituted by 1-3substituents selected from the group consisting of halogen, nitro,amino, mono(lower alkyl)amino, di(lower alkyl)amino, lower alkyl, loweralkoxy, benzyloxy, phenoxy, hydroxyl and trifluoromethyl; in whichsubstituents each alkyl chain or alkenyl chain can be interrupted byoxygen, sulfur or NR(8); R(8) is hydrogen, alkyl, cycloalkyl, arylalkyl,alkenyl, substituted aminoalkyl or an aryl or heteroaryl ring, whichrings are unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of halogen, nitro, amino, mono(lower alkyl)amino,di(lower alkyl)amino, lower alkyl, lower alkoxy, benzyloxy, phenoxy,hydroxyl and trifluoromethyl; or a pharmaceutically acceptable saltthereof; h) a compound of the formula

in which: R(1) is hydrogen, F, Cl, Br, I, —NO₂, —C≡N, —CF₃, R(4)—SO_(m)or R(5)R(6)N—SO₂—; m is zero, 1 or 2; R(4) and R(5) are (C₁-C₈)-alkyl,(C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(7) or CF₃; n is zero, 1, 2, 3 or 4; R(7)is (C₃-C₇)-cycloalkyl or phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(8)R(9); R(8) and R(9)  are H orC₁-C₄-alkyl; or R(5) is H; R(6) is H or (C₁-C₄)-alkyl; or R(5) and R(6)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl; R(2) is —SR(10), —OR(10),—NHR(10), —NR(10)R(11), —CHR(10)R(12), —[CR(12)R(13)OR(13′)],—{C—[CH₂—OR(13′)]R(12)(R(13)} or—[CR(18)R(17)]_(p)—(CO)—[CR(19)R(20)]_(q)—R(14); R(10) and R(11)identically or differently are—[CHR(16)]_(s)—(CH₂)_(p)—(CHOH)_(q)—(CH₂)_(r)—(CHOH)_(t)—R(21) or—(CH₂)_(p)—O—(CH₂—CH₂O)_(q)—R(21), R(21) is hydrogen, methyl, p, q, ridentically or differently are zero, 1, 2, 3 or 4; s is zero or 1; t is1, 2, 3 or 4; R(12) and R(13) identically or differently are hydrogen,(C₁-C₆)-alkyl or, together with the carbon atom carrying them, are a(C₃-C₈)-cycloalkyl, R(13′) is hydrogen or (C₁-C₄)-alkyl; R(14) is H,(C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or —C_(a)H_(2a)—R(15); a is zero, 1,2, 3 or 4; R(15) is phenyl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(8)R(9); R(8) and R(9)  are H or (C₁-C₄)-alkyl; or R(15)is (C₁-C₉)-heteroaryl, which is unsubstituted or substituted as phenyl,or R(15) is (C₁-C₆)-alkyl, which is unsubstituted or substituted by 1-3OH; R(16), R(17), R(18), R(19) and R(20) are hydrogen or (C₁-C₃)-alkyl;R(3) is defined as R(1), or R(3) is (C₁-C₆)-alkyl or —X—R(22); X isoxygen, S or NR(16); R(16) is H or (C₁-C₃)-alkyl; or R(22) and R(16)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl; or R(22) is defined asR(14); or a pharmaceutically tolerable salt thereof; i) abenzoylguanidine of the formula

in which: R(1) is hydrogen, F, Cl, Br, I, —NO₂, —C≡N,R(16)—C_(p)H_(2p)—O_(q), R(4)—SO_(m) or R(5)R(6)N—SO₂—; m is zero, 1 or2; p is, zero or 1; q is zero, 1, 2 or 3; R(16) is C_(r)F_(2r+1); r is1, 2 or 3; R(4) and R(5) are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl,—C_(n)H_(2n)—R(7) or CF₃; n is zero, 1, 2, 3 or 4; R(7) is(C₃-C₇)-cycloalkyl or phenyl, which is not substituted or is substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(8)R(9); R(8) and R(9)  are H or C₁-C₄-alkyl; orR(5) is H; R(6) is H or (C₁-C₄)-alkyl; or R(5) and R(6) together are 4or 5 methylene groups, of which one CH₂ group can be replaced by oxygen,S, NH, N—CH₃ or N-benzyl, R(2) is (C₁-C₉)-heteroaryl, which is linkedvia C or N and which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino; or R(2) is —SR(10),—OR(10), —NR(10)R(11), —CR(10)R(11)R(12); R(10) is—C_(a)H_(2a)—(C₁-C₉)-heteroaryl, which is unsubstituted or substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; a is zero,1 or 2; R(11) and R(12) independently of one another are defined asR(10) or are hydrogen or (C₁-C₄)-alkyl; R(3) is defined as R(1), or is(C₁-C₆)-alkyl or —X—R(13); X is oxygen, S, or NR(14); R(14) is H or(C₁-C₃)-alkyl; R(13) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(b)H_(2b)—R(15); b is zero, 1, 2, 3 or 4; or R(13) and R(14) togetherare 4 or 5 methylene groups, of which one CH₂ group can be replaced byoxygen, S, NH, N—CH₃ or N-benzyl; R(15) is phenyl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(8)R(9); R(8) and R(9) are H or (C₁-C₄)-alkyl; or a pharmaceutically tolerable salt thereof;k) a benzoylguanidine of the formula

in which: one of the substituents R(1), R(2), R(3) or R(4): is an aminogroup —NR(5)[C_(n)H_(2n)—R(6)]; R(5) is hydrogen or C₍₁₋₆₎-alkyl; n iszero, 1, 2, 3 or 4; R(6) is H or C₍₁₋₄₎-alkyl; in which one CH₂ groupcan be replaced by 1 sulfur atom or a group NR(7); R(7) is hydrogen,methyl or ethyl; or R(6) is C₍ ₃₋₈)-cycloalkyl or phenyl, which isunsubstituted or carries 1, 2 or 3 substituents selected from the groupconsisting of F, Cl, Br, methyl, methoxy, and —NR(8)R(9); R(8) and R(9) are H, methyl or ethyl; or R(5) and R(6) together with the nitrogenatom are a 5-, 6- or 7-membered ring, in which 1 carbon atom can bereplaced by oxygen, S or NR(10); R(10) is H, C₍₁₋₃₎-alkyl or benzyl; andthe other substituents R(1), R(2), R(3), R(4) in each case are:hydrogen, F, Cl, Br, I, CN, CF₃, NO₂, CF₃—O—, C_(m)F_(2m+1)—CH₂—O— orR(11)—C_(q)H_(2q)—X_(p)—; m is 1, 2 or 3; q is zero, 1, 2, 3 or 4; p iszero or 1; X is oxygen or NR(12); R(12) is H or C₍₁₋₃₎-alkyl; R(11) ishydrogen, C₍₁₋₆₎-alkyl, C₍₃₋₈₎-cycloalkyl or phenyl, which isunsubstituted or substituted by 1, 2 or 3 substituents selected from thegroup consisting of F, Cl, CH₃, CH₃—O— and NR(13)R(14); R(13) and R(14) are H, methyl or ethyl; or a pharmaceutically tolerable salt thereof;I) a benzoylguanidine of the formula

in which R(1) is R(4)R(5)N—C(X)—; X is oxygen, S or N—R(6); R(4) andR(5) identically or differently, are H, (C₁-C₈)-alkyl, (C₃-C₆)-alkenylor —C_(n)H_(2n)—R(7); n is zero, 1, 2, 3 or 4; R(7) is(C₅-C₇)-cycloalkyl or phenyl, which is unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methoxy and (C₁-C₄)-alkyl; or R(4) and R(5) together are 4 or 5methylene groups, of which one CH₂ group can be replaced by oxygen, S,NH, N—CH₃ or N-benzyl; R(6) is defined as R(4) or is amidine; R(2) is H,F, Cl, Br, I, (C₁-C₈)-alkyl, 1-alkenyl or 1-alkynyl, (C₃-C₈)-cycloalkyl,(C₃-C₈)-cycloalkyl-(C₁-C₄)-alkyl, phenyl, C₆H₅—(C₁-C₄)-alkyl, naphthyl,biphenylyl, 1,1-diphenyl-(C₁-C₄)-alkyl, cyclopentadienyl, pyridyl,thiopyridyl, pyrrolyl, furanyl, thienyl, thiazolyl, oxazolyl, indenyl,quinolyl, indolyl, benzofuranyl, benzothienyl, benzothiazolyl,benzoxazolyl or —W—R(8); W is oxygen, S or NR(9); R(8) is H,(C₁-C₆)-alkyl, (C₅-C₇)-cycloalkyl, cyclohexylmethyl, cyclopentylmethyl,—(CH₂)_(m)C_(p)F_(2p+1) or —C_(q)H_(2q)—R(10); m is zero or 1; p is 1, 2or 3; q is zero, 1, 2, 3 or 4; R(10) is phenyl, which is unsubstitutedor substituted by 1-3 substituents selected from the group consisting ofF, Cl, CF₃, methyl, methoxy and NR(11)R(12); R(11) and R(12)  are H or(C₁-C₄)-alkyl; R(9) is H or (C₁-C₃)-alkyl; or R(8) and R(9) together are4 or 5 methylene groups, of which one CH₂ group can be replaced byoxygen, S, NH, N—CH₃ or N-benzyl; R(3) is H, F, Cl, Br, I, (C₁-C₆)-alkylor —W—R(8) as defined for R(2), or a pharmaceutically acceptable saltthereof; m) a benzoylguanidine of the formula

in which: R(1), R(2), R(3) are hydrogen, F, Cl, Br, I or (C₁-C₁₂)-alkyl;one of the substituents R(1), R(2) or R(3) is N₃, CN, OH or(C₁-C₁₀)-alkyloxy, if at least one of the remaining substituents R(1),R(2) or R(3) is a sufficiently lipophilic alkyl radical having 3 to 12carbon atoms; or one of the substituents R(1), R(2) or R(3) isR(4)—C_(n)H_(2n)—O_(m)—, m is zero or 1; n is zero, 1, 2 or 3; R(4) isC_(p)F_(2p+1); p is 1, 2 or 3, if n is zero or 1; or R(4) is(C₃-C₁₂)-cycloalkyl, phenyl, pyridyl, quinolyl or isoquinolyl, where thearomatic and heteroaromatic ring systems are unsubstituted orsubstituted by a substituent selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(5)R(6); R(5) and R(6) are hydrogen or(C₁-C₄)-alkyl; or one of the substituents R(1), R(2) or R(3) is —C≡CR(5)or —C[R(6)]=CR(5); R(5) is phenyl, which is unsubstituted or substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy, hydroxyl, amino, methylamino and dimethylamino, and(C₁-C₉)-heteroaryl, which is unsubstituted or substituted as phenyl, orR(5) is (C₁-C₆)-alkyl, which is unsubstituted or substituted by 1-3 OH;or R(5) is (C₃-C₈)-cycloalkyl, R(6) is hydrogen or methyl; or apharmacologically acceptable salt thereof; o) a benzoylguanidine of theformula

in which: R(1) is hydrogen, F, Cl, Br, I, —NO₂, —C≡N,X_(o)—(CH₂)_(p)—(CF₂)_(q)—CF₃, R(5)—SO_(m), R(6)—CO— or R(6)R(7)N—SO₂—,where X is oxygen, S or NR(14); m is zero, 1 or 2; o is zero or 1; p iszero, 1 or 2; q is zero, 1, 2, 3, 4, 5 or 6; R(5) and R(6) are(C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(8) or CF₃; n is zero, 1,2, 3 or 4; R(8) is (C₃-C₇)-cycloalkyl or phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(9)R(10); R(9) andR(10)  are H or C₁-C₄-alkyl; or R(6) is H; R(7) is H or (C₁-C₄)-alkyl;or R(6) and R(7) together are 4 or 5 methylene groups, of which one CH₂group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl;

Y is oxygen, —S— or —NR(12)—;  R(11) and R(12)  are hydrogen or(C₁-C₃)-alkyl; h is zero or 1; i, j and k  independently are zero, 1, 2,3 or 4; but where h, i and k are not simultaneously zero, R(3) isdefined as R(1), or is (C₁-C₆)-alkyl or —X—R(13); X is oxygen, S orNR(14); R(14) is H or (C₁-C₃)-alkyl; R(13) is H, (C₁-C₆)-alkyl,(C₃-C₈)-cycloalkyl or —C_(b)H_(2b)—R(15); b is zero, 1, 2, 3 or 4; orR(13) and R(14)  together are 4 or 5 methylene groups, where one CH₂group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl;  R(15) isphenyl,  which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(9)R(10);  R(9) and R(10)  are H or (C₁-C₄)-alkyl; R(4) is hydrogen,—OR(16) or —NR(16)R(17); R(16) and R(17) independently are hydrogen or(C₁-C₃)-alkyl; or a pharmaceutically tolerable salt thereof; p) abenzoylguanidine of the formula

in which: R(1) is R(6)—CO or R(7)R(8)N—CO; R(6) is (C₁-C₆)-alkyl,(C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or —C_(n)H_(2n)—R(9); n is zero,1, 2, 3 or 4; R(9) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl ornaphthyl, where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(10)R(11); R(10) and R(11)  are H, (C₁-C₄)-alkylor (C₁-C₄)-perfluoro-alkyl; R(7) is H, (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or —C_(n)H_(2n)—R(12); n iszero, 1, 2, 3 or 4; R(12) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl ornaphthyl, where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(13)R(14); R(13) and R(14)  are H, (C₁-C₄)-alkylor (C₁-C₄)-perfluoro-alkyl; R(8) is H, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; or R(7) and R(8) together are 4 or 5 methylenegroups, of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃or N-benzyl; R(2) is defined as R(1), or is H, F, Cl, Br, I, CN, NO₂,(C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(n)H_(2n)—R(15); n is zero,1, 2, 3 or 4; R(15) is (C₃-C₈)-cycloalkyl,phenyl, biphenylyl or naphthyl, where the aromatics are not substitutedor are substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(16)R(17); R(16) andR(17)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoro-alkyl; or R(2) is(C₁-C₉)-heteroaryl, which is linked via C or N and which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; or R(2) is SR(18), —OR(18), —NR(18)R(19) or—CR(18)R(19)R(20); R(18) is —C_(a)H_(2a)—(C₁-C₉)-heteroaryl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; a is zero, 1 or 2; R(19) and R(20) independently of oneanother are defined as R(18) or are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; or R(2) is R(21)—SO_(m) or R(22)R(23)N—SO₂—; mis 1 or 2; R(21) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₉)-alkenyl or —C_(n)H_(2n)—R(24), n is zero, 1, 2, 3 or 4; R(24) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(27)R(28);R(27) and R(28)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoro-alkyl; R(22)is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(n)H_(2n)—R(29); n is zero, 1, 2, 3 or 4; R(29) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(30)R(31);R(30) and R(31)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoro-alkyl; R(23)is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; or R(22) and R(23)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl; or R(2) is R(33)X—; X isoxygen, S, NR(34), (D═O)A—, NR(34)C═MN^((*))R(35)—; M is oxygen or S; Ais oxygen or NR(34); D is C or SO; R(33) is (C₁-C₈)-alkyl,(C₃-C₈)-alkenyl, (CH₂)_(b)C_(d)F_(2d+1) or —C_(n)H_(2n)—R(36), b is zeroor 1; d is 1, 2, 3, 4, 5, 6 or 7; n is zero, 1, 2, 3 or 4; R(36) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(37)R(38);R(37) and R(38)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoro-alkyl; R(34)is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(35) is defined asR(33); or R(33) and R(34) together are 4 or 5 methylene groups, of whichone CH₂ group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl; where A and N^((*)) are bonded to the phenyl nucleus of thebenzoylguanidine parent structure; or R(2) is —SR(40), —OR(40),—NHR(40), —NR(40)R(41), —CHR(40)R(42), —C[R(42)R(43)OH], —C≡CR(45),—CR(46)═CHR(45) or —[CR(47)R(48)]_(u)—(CO)—[CR(49)R(50)]_(v)—R(44);R(40), R(41) identically or differently are—(CH₂)_(p)—(CHOH)_(q)—(CH₂)_(r)—(CHOH)_(t)—R(51) or—(CH₂)_(p)—O—(CH₂-CH₂O)_(q)—R(51); R(51) is hydrogen or methyl; u is 1,2, 3 or 4; v is zero, 1, 2, 3 or 4; p, q, r identically or differentlyare zero, 1, 2, 3 or 4; t is 1, 2, 3 or 4; R(42) and R(43) identicallyor differently are hydrogen or (C₁-C₆)-alkyl; or R(42) and R(43)together with the carbon atom carrying them form a (C₃-C₈)-cycloalkyl;R(44) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or —C_(e)H_(2e)—R(45); eis zero, 1, 2, 3 or 4; R(45) is phenyl, which is unsubstituted orsubstituted by 1-3 substituents from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(52)R(53) where  R(52) and R(53) are H or(C₁-C₄)-alkyl, or R(45) is (C₁-C₉)-heteroaryl, which is unsubstituted orsubstituted as phenyl; or R(45) is (C₁-C₆)-alkyl, which is unsubstitutedor substituted by 1-3 OH; R(46), R(47), R(48), R(49) and R(50) arehydrogen or methyl; or R(2) is R(55)—NH—SO₂—; R(55) isR(56)R(57)N—(C═Y)—; Y is oxygen, S or N—R(58); R(56) and R(57)identically or differently are H, (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl or—C_(f)H_(2f)—R(59); f is zero,1, 2, 3 or 4; R(59) is (C₅-C₇)-cycloalkylor phenyl,  which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methoxy and(C₁-C₄)-alkyl; or R(56) and R(57) together are 4 or 5 methylene groups,of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃ orN-benzyl; R(58) is defined as R(56) or is amidine; R(3), R(4) and R(5)independently of one another are defined as R(1) or R(2); or apharmaceutically tolerable salt thereof; q) a benzoylguanidine of theformula

in which: R(1) is hydrogen, F, Cl, Br, I, —NO₂, —C≡N,—X_(o)—(CH₂)_(p)—(CF₂)_(q)—CF₃, R(5)—SO_(m)—, R(6)—CO—, R(6)R(7)N—CO— orR(6)R(7)N—SO₂—; X is oxygen, —S—or NR(14); m is zero, 1 or 2; o is zeroor 1; p is zero, 1 or 2; q is zero, 1, 2, 3, 4, 5 or 6; R(5) and R(6)are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(8) or CF₃; n is zero,1, 2, 3 or 4; R(8) is (C₃-C₇)-cycloalkyl, phenyl, which is notsubstituted or is substituted by 1 to 3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(9)R(10); R(9) andR(10)  are H or (C₁-C₄)-alkyl; or R(6) is hydrogen; R(7) is hydrogen or(C₁-C₄)-alkyl; or R(6) and R(7) together are 4 or 5 methylene groups, ofwhich one CH₂ group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl;R(2) is

R(11) is (C₁-C₉)-heteroaryl, which is linked via C or N and which isunsubstituted or substituted by 1 to 3 substituents selected from thegroup consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino, dimethylamino and benzyl; Y is oxygen, —S—or NR(12); R(12)is H or (C₁-C₄)-alkyl; R(3) is defined as R(1); or R(3) is (C₁-C₆)-alkylor —X—R(13); X is oxygen, —S— or NR(14); R(14) is H or (C₁-C₃)-alkyl;R(13) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or —C_(b)H_(2b)—R(15); bis zero, 1, 2, 3 or 4; or R(13) and R(14) together are 4 or 5 methylenegroups, of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃or N-benzyl; R(15) is phenyl, which is unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(9)R(10); R(9) and R(10)  are H or (C₁-C₄)-alkyl;R(4) is hydrogen, —OR(16), —NR(16)R(17) or C_(r)F_(2r+1); R(16) andR(17) independently are hydrogen or (C₁-C₃)-alkyl; r is 1, 2, 3 or 4; ora pharmaceutically tolerable salt thereof; r) a benzo-fused 5-memberedring heterocycle of the formula

in which: X is N or CR(6); Y is oxygen, S or NR(7); A, B together are abond or A, B are both hydrogen, if X is CR(6) and Y is NR(7)simultaneously; one of the substituents R(1) to R(6) is a —CO—N═C(NH₂)₂group; the other substituents R(1) to R(6) in each case are hydrogen, F,Cl, Br, I or (C₁-C₉)-alkyl; up to two of the other substituents R(1) toR(6) are CN, NO₂, N₃, (C₁-C₄)-alkyloxy or CF₃; up to one of the othersubstituents is R(8)—C_(n)H_(2n)—Z—; n is zero to 10; where the alkylenechain —C_(n)H_(2n)— is straight-chain or branched and where one carbonatom can be replaced by an oxygen or sulfur atom or by a nitrogen atom;R(8) is hydrogen, (C₂-C₆)-alkenyl or (C₃-C₁₀)-cycloalkyl, which isunsubstituted or substituted by 1 to 4 methyl groups or an OH group, orcan contain an ethylene group —CH═CH—, and in which one methylene groupcan be replaced by an oxygen or sulfur atom or by a nitrogen atom; orR(8) is phenyl, which is unsubstituted or substituted by 1 to 3substituents selected from the group consisting of F, Cl, Br, I, CF₃,CH₃—S(O)_(s)— or R(9)—W_(y)—; s is zero, 1 or 2; R(9) is H, methyl,ethyl, W is oxygen or NR(10); R(10) is H or methyl; y is zero or 1; orR(8) is C_(m)F_(2m+1); m is 1 to 3; or R(8) is 1- or 2-naphthyl,pyridyl, quinolyl or isoquinolyl; Z is —CO—, —CH₂— or—[CR(11)(OH)]_(q)—; q is 1, 2 or 3; R(11) is H or methyl; or Z is oxygenor —NR(12)—; R(12) is H or methyl; or Z is —S(O)_(s)—; s is zero, 1 or2; or Z is —SO₂—NR(13)—; R(13) is H or (C₁-C₄)-alkyl; R(7) is hydrogen,(C₁-C₁₀)-alkyl, (C₂-C₁₀)-alkenyl or R(8)—C_(n)H_(2n)—; or apharmaceutically tolerable salt thereof; s) a benzoylguanidine of theformula

in which: R(1), R(3) or R(4) is —NR(6) C═X NR(7)R(8); X is oxygen or S;R(6) is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenylor —C_(n)H_(2n)—R(9); n is zero, 1, 2, 3 or 4; R(9) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,  where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(10)R(11); R(10) and R(11)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(7)is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(o)H_(2o)—R(12); o is zero, 1, 2, 3 or 4; R(12) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(13)R(14);R(13) and R(14)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(8) isdefined as R(7); or R(7) and R(8) together are 4 or 5 methylene groups,of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃ orN-benzyl; the remaining substituents R(2), R(3), R(4), R(5) or R(1),R(2), R(4), R(5) or R(1), R(2), R(3), R(5) in each case independently ofone another are hydrogen, F, Cl, Br, I, —O_(ta)(C₁-C₈)-alkyl,—O_(tb)(C₃-C₈)-alkenyl, —O_(tc)(CH₂)_(b)C_(d)F_(2d+1),—O_(td)C_(p)H_(2p)R(18), or up to 2 groups CN, NO₂, NR(16)R(17), b iszero or 1; d is 1, 2, 3, 4, 5, 6 or 7; ta is zero or 1; tb is zero or 1;tc is zero or 1; td is zero or 1; p is zero, 1, 2, 3 or 4; R(18) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(19)R(20);R(19) and R(20) are hydrogen or (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;R(16) is hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(q)H₂q-R(21), q is zero,1, 2, 3 or 4; R(21) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents from thegroup F, Cl, CF₃, methyl, methoxy or NR(22)R(23), R(22) and R(23) arehydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(17) is hydrogen,(C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(r)H_(2r)—R(24); r is zero, 1, 2, 3 or 4; R(24) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(25)R(26);R(25) and R(26)  are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;or R(16) and R(17) together are 4 or 5 methylene groups, of which oneCH₂ group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl; or apharmaceutically tolerable salt thereof; t) a diacyl-substitutedguanidine of the formula

in which: X(1) and X(2) are

T1 is zero, 1, 2, 3 or 4; R(A) and R(B) independently of one another arehydrogen, F, Cl, Br, I, CN, OR(106), (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl,O_(zk)(CH₂)_(zl)C_(zm)F_(2zm+1), NR(107)R(108), phenyl or benzyl, wherethe aromatics are not substituted or are substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(109)R(10); R(109) and R(110)  are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; zl is zero, 1, 2, 3 or 4; zk is zero or 1; zm is1, 2, 3,4, 5, 6, 7 or 8; R(106) is hydrogen, (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl, (C₃-C₈)-cycloalkyl, phenyl orbenzyl,  where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(111)R(112);  R(11) and R(112)  are hydrogen,(C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(107) and R(108) independentlyof one another are defined as R(106), or R(107) and R(108) together are4 or 5 methylene groups, of which one CH₂ group can be replaced byoxygen, S, NH, N—CH₃ or N-benzyl; or X(1) and X(2) are

T2a and T2b independently of one another are zero, 1 or 2; where thedouble bond can have the (E)- or (Z)-configuration; or X(1) and X(2) are

T3 is zero, 1 or 2; U, YY and Z independently of one another are C or N,where U, YY, Z can carry the following number of substituents: Bonded inthe ring to Number of permitted U, YY or Z a double bond substituents Cyes 1 C no 2 N yes 0 N no 1

R(D) is hydrogen, (C₁-C₈)-alkyl or (C₁-C₈)-perfluoroalkyl, R(U1), R(U2),R(Y1), R(Y2), R(Z1), R(Z2) independently of one another are hydrogen, F,Cl, Br, I, CN, OR(114), (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl,O_(zka)(CH₂)_(zla)C_(zma)F_(2zma+1), NR(115)R(116), phenyl or benzyl,where the aromatics are not substituted or are substituted by 1-3substituents -selected from the group consisting of F, Cl, CF₃, methyl,methoxy, and NR(117)R(118), R(117) and R(118)  are hydrogen,(C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl, zka is zero or 1; zla is zero,1, 2, 3 or 4; zma is 1, 2, 3, 4, 5, 6, 7 or 8; R(114) is hydrogen,(C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl,(C₃-C₈)-cycloalkyl, phenyl or benzyl,  where the aromatics are notsubstituted or are substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(119)R(120); R(119) and R(120)  are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoro-alkyl; R(115) and R(116) independently of one anotherare defined as R(114); or R(115) and R(116) together are 4 or 5methylene groups, of which one CH₂ group can be replaced by oxygen, S,NH, N—CH₃ or N-benzyl; but where the constitution of U is nitrogen (N),YY is nitrogen (N) and Z is carbon (C) is excluded, R(101), R(102),R(103), R(104) and R(105) independently of one another are hydrogen, F,Cl, Br, I, —C≡N, X_(zoa)-(CH₂)_(zqa)-(C_(zqa)F₂₊₁), R(110a)—SO_(zbm),R(110b)R(110c)N—CO, R(111a)—CO— or R(112a)R(113a)N—SO₂—, where theperfluoroalkyl group is straight-chain or branched, X is oxygen, S orNR(114a); R(114a)  is H or (C₁-C₃)-alkyl; zoa is zero or 1; zbm is zero,1 or 2; zpa is zero, 1, 2, 3 or 4; zqa is 1, 2, 3,4, 5, 6, 7 or 8;R(110a), R(110b), R(111a) and R(112a) independently of one another are(C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, —C_(zn)H_(2zn)—R(115a) or(C₁-C₈)-perfluoroalkyl; zn is zero, 1, 2, 3 or 4; R(115a)  is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(116a)R(117a); R(116a) and R(117a)  are hydrogen, (C₁-C₄)-perfluoroalkyl or(C₁-C₄)-alkyl; or R(110b), R(111a) and R(112a) are hydrogen; R(110c) andR(113a) independently are hydrogen, (C₁-C₄)-perfluoroalkyl or(C₁-C₄)-alkyl; or R(110b) and R(110c) and R(112a) and R(113a) togetherare 4 or 5 methylene groups, of which one CH₂ group can be replaced byoxygen, sulfur, NH, N—CH₃ or N-benzyl; or R(101), R(102), R(103),R(104), R(105) independently of one another are (C₁-C₈)-alkyl,—C_(zal)H_(2zal)R(118a) or (C₃-C₈)-alkenyl, zal is zero, 1, 2, 3 or 4;R(118a) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,  wherethe aromatics are not substituted or are substituted by 1-3 substituentsfrom the group consisting of F, Cl, CF₃, methyl, methoxy orNR(119a)R(119b);  R(119a) and R(119b)  are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; or R(101), R(102), R(103), R(104), R(105)independently of one another are (C₁-C₉)-heteroaryl, which is linked viaC or N and which is unsubstituted or substituted by 1-3 substituentsfrom the group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; or R(101), R(102), R(103), R(104), R(105)independently of one another are —C≡C—R(193); R(193) is phenyl which isnot substituted or is substituted by 1-3 substituents from the groupconsisting of F, Cl, CF₃, methyl, methoxy or NR(194)R(195); R(194) andR(195)  are hydrogen or CH₃; or R(101), R(102), R(103), R(104), R(105)independently of one another are—Y-para-C₆H₄—(CO)_(zh)—(CHOH)_(zi)—(CH₂)_(zj)—(CHOH)_(zk)—R(123),—Y-meta-C₆H₄—(CO)_(zad)—(CHOH)_(zae)—(CH₂)_(zaf)—(CHOH)_(zag)—R(124) or—Y-Ortho-C₆H₄—(CO)_(zah)—(CHOH)_(zao)—(CH₂)_(zap)—(CHOH)_(zak)—R(125); Yis oxygen, —S— or —NR(122d)—; zh, zad, zah independently are zero or 1;zi, zj, zk, zae, zaf, zag, zao, zap and zak independently are zero, 1,2, 3 or 4; but where in each case zh, zi and zk are not simultaneouslyzero, zad, zae and zag are not simultaneously zero, and zah, zao and zakare not simultaneously zero, R(123), R(124), R(125) and R(122d)independently are hydrogen or (C₁-C₃)-alkyl; or R(101), R(102), R(103),R(104) and R(105) independently of one another are SR(129), —OR(130),—NR(131)R(132) or —CR(133)R(134)R(135); R(129), R(130), R(131) andR(133) independently are —C_(zab)H_(2zab)—(C₁-C₉)-heteroaryl,  which isunsubstituted or substituted by 1-3 substituents from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; zab is zero, 1 or 2; R(132), R(134) and R(135) independently of one another are defined as R(129) or are hydrogen,(C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; or R(101), R(102), R(103),R(104) and R(105) independently of one another are—W-para-(C₆H₄)—R(196), —W-meta-(C₆H₄)—R(197) or —W-ortho-(C₆H₄)—R(198);R(196), R(197) and R(198) independently are (C₁-C₉)-heteroaryl,  whichis linked via C or N and which is unsubstituted or substituted by 1 to 3substituents from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino, dimethylamino and benzyl; W is oxygen, Sor NR(136)—; R(136)  is hydrogen or (C₁-C₄)-alkyl; or R(101), R(102),R(103), R(104) and R(105) independently of one another are R(146)X(1a)—;X(1a) is oxygen, S, NR(147), (D═O)A—, NR(148)C═MN^((*))R(149)—; M isoxygen or sulfur; A is oxygen or NR(150); D is C or SO; R(146) is(C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, (CH₂)_(zbz)C_(zdz)F_(2dz+1) or—C_(zxa)H_(2zxa)—R(151); zbz is zero or 1; zdz is 1, 2, 3, 4, 5, 6 or 7;zxa is zero, 1, 2, 3 or 4; R(151) is (C₃-C₈)-cycloalkyl, phenyl,biphenylyl or naphthyl,  where the aromatics are not substituted or aresubstituted by 1-3 substituents from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(152)R(153); R(152) and R(153) are hydrogen,(C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(147), R(148) and R(150)independently are hydrogen, (C₁-C₄)-alkyl, (C₁-C₄)-perfluoroalkyl;R(149) is defined as R(146), or R(146) and R(147), or R(146) and R(148)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;  where A and N^((*))are bonded to the phenyl nucleus of the alkanoyl parent structure; orR(101), R(102), R(103), R(104) and R(105) independently of one anotherare —SR(164), —OR(165), —NHR(166), —NR(167)R(168), —CHR(169)R(170),—CR(154)R(155)OH, —C≡CR(156), —CR(158)═CR(157) or—[CR(159)R(160)]_(zu)—(C═O)—[CR(161)R(162)]_(zv)—R(163); R(164), R(165),R(166), R(167), R(169) identically or differently are—(CH₂)_(zy)—(CHOH)_(zz)—(CH₂)_(zaa)—(CHOH)_(zt)—R(171) or—(CH₂)_(zab)—O—(CH₂-CH₂O)_(zac—R()172); R(171) and R(172)  are hydrogenor methyl; zu is 1, 2, 3 or 4; zv is zero, 1, 2, 3 or 4; zy, zz, zaa,zab, zac  identically or differently are zero, 1, 2, 3 or 4; zt is 1, 2,3 or 4; R(168), R(170), R(154), R(155) identically or differently arehydrogen or (C₁-C₆)-alkyl, or R(169) and R(170), or R(154) and R(155)together with the carbon.atom carrying them are a (C₃-C₈)-cycloalkyl;R(163) is hydrogen, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or—C_(zeb)H_(2zeb)—R(173); zeb is zero, 1, 2, 3 or 4; R(156), R(157) andR(173)  independently are phenyl which is unsubstituted or issubstituted by 1-3 substituents from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(174)R(175);  R(174) and R(175)  hydrogen or(C₁-C₄)-alkyl; or R(156), R(157) and R(173) independently are(C₁-C₉)-heteroaryl,  which is unsubstituted or substituted as phenyl;R(158), R(159), R(160), R(161) and R(162) are hydrogen or methyl, orR(101), R(102), R(103), R(104), R(105) independently of one another areR(176)—NH—SO₂—; R(176) is R(177)R(178)N—(C═Y′)—; Y′ is oxygen, S orN—R(179); R(177) and R(178) identically or differently are hydrogen,(C₁-C₈)-alkyl, (C₃-C₆)-alkenyl or —C_(zfa)H_(2zfa)—R(180); zfa is zero,1, 2, 3 or 4; R(180)  is (C₅-C₇)-cycloalkyl or phenyl,  which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methoxy and (C₁-C₄)-alkyl; or R(177) andR(178) together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl; R(179) is definedas R(177) or is amidine, or R(101), R(102), R(103), R(104), R(105)independently of one another are NR(184a)R(185), OR(184b), SR(184c) or—C_(znx)H_(2znx)—R(184d); znx is zero, 1, 2, 3 or 4; R(184d) is(C₃-C₇)-cycloalkyl or phenyl, which is not substituted or is substitutedby 1-3 substituents from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(116k)R(117k); R(116k) and R(117k)  are hydrogen orC₁-C₄-alkyl; R(184a), R(184b), R(184c), R(185) independently of oneanother are hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl or(CH₂)_(zao)—R(184g); zao is zero, 1, 2, 3 or 4; R(184g) is(C₃-C₇)-cycloalkyl or phenyl,  which is not substituted or issubstituted by 1-3 substituents from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(184u)R(184v);  R(184u) and R(184v)  are hydrogenor C₁-C₄-alkyl;  or  R(184a) and R(185)  together are 4 or 5 methylenegroups, of  which one CH₂ group can be replaced by oxygen, sulfur, NH,N—CH₃ or N-benzyl; or a pharmaceutically tolerable salt thereof; u) abenzoylguanidine of the formula

in which: R(1) is H, F, Cl, Br, I, CN, NO₂, (C₁-C₈)-alkyl,(C₃-C₈)-cycloalkyl or X_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃; X is oxygen, S orNR(5); a is zero or 1; b is zero, 1 or 2; c is zero, 1, 2 or 3; R(5) isH, (C₁-C₄)-alkyl or —C_(d)H_(2d)R(6); d is zero, 1, 2, 3 or 4; R(6) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,  where the aromaticsare not substituted or are substituted by 1 to 3 substituents selectedfrom the group consisting of F, Cl, CF₃, methyl, methoxy and NR(7)R(8); R(7) and R(8)  independently are H or (C₁-C₄)-alkyl; or R(1) is—SR(10), —OR(10) or —CR(10)R(11)R(12); R(10) is—C_(f)H_(2f)—(C₃-C₈)-cycloalkyl, —(C₁-C₉)-heteroaryl or phenyl, wherethe aromatic systems are unsubstituted or substituted by 1 to 3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; f is zero, 1 or2; R(11) and R(12) independently of one another are defined as R(10) orare hydrogen or (C₁-C₄)-alkyl; or R(1) is phenyl, naphthyl, biphenylylor (C₁-C₉)-heteroaryl, the latter linked via C or N, and which areunsubstituted or substituted by 1 to 3 substituents selected from thegroup consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; or R(1) is —SR(13), —OR(13), —NHR(13),—NR(13)R(14), —CHR(13)R(15), —C[R(15)R(16)]OH, —C≡CR(18),—C[R(19)]=CR(18) or —[CR(20)R(21)]_(k)—(CO)—[CR(22)R(23)R(24)]_(l) R(13)and R(14) identically or differently are—(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(j)—(CHOH)_(j)—R(17), R(17) is hydrogen ormethyl; or —(CH₂)_(g)—O—(CH₂-CH₂O )_(h)—R(24), g, h, i identically ordifferently are zero, 1, 2, 3 or 4; J is 1, 2, 3 or 4; R(15) and R(16)identically or differently are hydrogen, (C₁-C₆)-alkyl or together withthe carbon atom carrying them are a (C₃-C₈)-cycloalkyl; R(18) is phenyl,which is unsubstituted or substituted by 1 to 3 substituents selectedfrom the group consisting of F, Cl, CF₃, methyl, methoxy andNR(25)R(26); R(25) and R(26) are H or (C₁-C₄)-alkyl; or R(18) is(C₁-C₉)-heteroaryl, which is unsubstituted or substituted as phenyl; orR(18) is (C₁-C₆)-alkyl, which is unsubstituted or substituted by 1 to 3OH; or R(18) is (C₃-C₈)-cycloalkyl; R(19), R(20), R(21), R(22) and R(23)are hydrogen or methyl; k is zero, 1, 2, 3 or 4; l is zero, 1, 2, 3 or4; R(24) is H, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or —C_(m)H_(2m)—R(18);m is 1, 2, 3 or 4; R(2) and R(3) independently of one another aredefined as R(1); R(4) is (C₁-C₃)-alkyl, F, Cl, Br, I, CN or—(CH₂)_(n)—(CF₂)_(o)—CF₃; n is zero or 1; o is zero, 1 or 2; or apharmaceutically tolerable salt thereof; v) an acylguanidine of theformula

in which: X is carbonyl or sulfonyl, R(1) is H or (C₁-C₈)-alkyl,unsubstituted or substituted by hydroxyl, (C₃-C₈)-cycloalkyl or phenyl,which is unsubstituted or substituted by 1-3 substituents from the groupF, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino, R(2) is H or (C₁-C₄)-alkyl, or a pharmaceuticallytolerable salt thereof; w) a phenyl-substituted alkylcarboxylic acidguanidide of the formula

in which: R(A) is hydrogen, F, Cl, Br, I, CN, OR(6), (C₁-C₈)-alkyl,(C₃-C₈)-cycloalkyl, O_(r)(CH₂)_(a)C_(b)F_(2b+1) or NR(7)R(8); r is zeroor 1; a is zero, 1, 2, 3 or 4; b is 1, 2, 3,4, 5, 6, 7 or 8; R(6) ishydrogen, (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, (C₃-C₈)-cycloalkyl, phenyl orbenzyl, where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(9)R(10); R(9) and R(10) are H, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; R(7) and R(8) independently of one another aredefined as R(6); R(B) independently is defined as R(A); X is 1, 2 or 3;R(1) is hydrogen, (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl,—O_(t)(CH₂)_(d)C_(e)F_(2e+1), F, Cl, Br, I or CN; t is zero or 1; d iszero, 1, 2, 3 or 4; e is 1, 2, 3, 4, 5, 6, 7 or 8; R(2), R(3), R(4) andR(5) independently of one another are defined as R(1); but with thecondition that at least one of the substituents R(1), R(2), R(3), R(4),R(5), R(A) and R(B) is an —O_(t)(CH₂)_(d)C_(e)F_(2e+1) or anO_(r)(CH₂)_(a)C_(b)F_(2b+1) group, or a pharmaceutically tolerable saltthereof; x) a heteroaroylguanidine of the formula

in which: HA is SO_(m), O or NR(5); m is zero, 1 or 2; R(5) is hydrogen,(C₁-C₈)-alkyl or —C_(am)H_(2am)R(81); am is zero, 1 or 2; R(81) is(C₃-C₈)-cycloalkyl or phenyl, which is not substituted or is substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(82)R(83); (82) and R(83)  are H or CH₃; or R(81)is (C₁-C₉)-heteroaryl, which is linked via C or N and which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; one of the two substituents R(1) and R(2) is—CO—N═C(NH₂)₂; and the other in each case is hydrogen, F, Cl, Br, I,(C₁-C₃)-alkyl, —OR(6), C_(r)F_(2r+1), —CO—N═C(NH₂)₂ or —NR(6)R(7); R(6)and R(7) independently are hydrogen or (C₁-C₃)-alkyl; r is 1, 2, 3 or 4;R(3) and R(4) independently of one another are hydrogen, F, Cl, Br, I,—C≡N, X—(CH₂)_(p)—(C_(q)—F_(2q+1)), R(8)—SO_(bm), R(9)R(10)N—CO,R(11)—CO— or R(12)R(13)N—SO₂—, where the perfluoroalkyl group isstraight-chain or branched, X is oxygen, S or NR(14); R(14) is H or(C₁-C₃)-alkyl; bm is zero, 1 or 2; p is zero, 1 or 2; q is zero, 1, 2,3, 4, 5 or 6; R(8), R(9), R(11) and R(12) independently are(C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(15) or CF₃; n is zero, 1,2, 3 or 4; R(15) is (C₃-C₇)-cycloalkyl or phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(16)R(17); R(16)and R(17)  are H or C₁-C₄-alkyl; or R(9), R(11) and R(12) are H; R(10)and R(13) independently are H or (C₁-C₄)-alkyl; or R(9) and R(10), andR(12) and R(13) together are 4 or 5 methylene groups, of which one CH₂group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl, or R(3) andR(4) independently of one another are (C₁-C₈)-alkyl or—C_(al)H_(2al)R(18); al is zero, 1 or 2; R(18) is (C₃-C₈)-cycloalkyl orphenyl; which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(19)R(20); R(19) and R(20) are H or CH₃; or R(3) and R(4)independently of one another are (C₁-C₉)-heteroaryl, which is linked viaC or N and which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, CH₃, methoxy,hydroxyl, amino, methylamino and dimethylamino; or R(3) and R(4)independently of one another are

 or Y is oxygen, —S— or —NR(22)—; h, ad, ah independently are zero or 1;i, j, k, ae, af, ag, ao, ap and ak independently are zero, 1, 2, 3 or 4,but where in each case h, i and k are not simultaneously zero, ad, aeand ag are not simultaneously zero, ah, ao and ak are not simultaneouslyzero, R(23), R(24), R(25) and R(22) independently are hydrogen or(C₁-C₃)-alkyl; or R(3) and R(4) independently of one another arehydrogen, F, Cl, Br, I, CN, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(g)H_(2g)R(26); g is zero, 1, 2, 3 or 4; R(26) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(27)R(28);R(27) and R(28) are H, (C₁-C₄)-alkyl or (C₁-C₄)-pefluoroalkyl; or R(3)and R(4) independently of one another are SR(29), —OR(30), —NR(31)R(32)or —CR(33)R(34)R(35); R(29), R(30), R(31) and R(33) independently are—C_(a)H_(2a)—(C₁-C₉)-heteroaryl, which is unsubstituted or substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; a is zero,1 or 2; R(32), R(34) and R(35) independently of one another are definedas R(29) or are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; orR(3) and R(4) independently of one another are

R(96), R(97) and R(98) independently are (C₁-C₉)-heteroaryl,  which islinked via C or N and which is unsubstituted or substituted by 1 to 3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino, dimethylamino or benzyl; W isoxygen, S or NR(36)—; R(36) is H or (C₁-C₄)-alkyl; or R(3) and R(4)independently of one another are R(37)—SO_(cm) or R(38)R(39)N—SO₂—; cmis 1 or 2; R(37) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(s)H_(2s)R(40); s is zero, 1, 2, 3 or 4; R(40) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(41)R(42);R(41) and R(42)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(38)is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(w)H_(2w)—R(43); w is zero, 1, 2, 3 or 4; R(43) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(44)R(45);R(44) and R(45)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(39)is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; or R(38) and R(39)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl; or R(3) and R(4)independently of one another are R(46)X(1)—; X(1) is oxygen, S, NR(47),(D═O)A— or NR(48)C═MN^((*))R(49)—, M is oxygen or S; A is oxygen orNR(50); D is C or SO; R(46) is (C₁-C₈)-alkyl, (C₃-C₈)-alkenyl,(CH₂)_(b)C_(d)F_(2d+1) or —C_(x)H_(2x)—R(51); b is zero or 1; d is 1, 2,3, 4, 5, 6 or 7; x is zero, 1, 2, 3 or 4; R(51) is (C₃-C₈)-cycloalkyl,phenyl, biphenylyl or naphthyl, where the aromatics are not substitutedor are substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(52)R(53); R(52); andR(53) are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(47), R(48) andR(50) independently are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; R(49) is defined as R(46); or R(46) and R(47),or R(46) and R(48) together are 4 or 5 methylene groups, of which oneCH₂ group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl, where Aand N^((*)) are bonded to the phenyl nucleus of the benzoylguanidineparent structure; or R(3) and R(4) independently of one another are—SR(64), —OR(65), —NHR(66), —NR(67)R(68), —CHR(69)R(70),—C(OH)R(54)R(55), —C≡CR(56), —CR(58)═CH R(57) or—[CR(59)R(60)]_(u)—(CO)—[CR(61)R(62)]_(v)—R(63); R(64), R(65), R(66),R(67) and R(69) identically or differently are—(CH₂)_(y)—(CHOH)_(z)—(CH₂)_(aa)—(CH₂OH)_(t)—R(71) or—(CH₂)_(ab)—O—(CH₂—CH₂O)_(ac)—R(72), R(71) and R(72) are hydrogen ormethyl; u is 1, 2, 3 or 4; v is zero, 1, 2, 3 or 4; y, z, aa, ab and acidentically or differently are zero, 1, 2, 3 or 4; t is 1, 2, 3 or 4;R(68), R(70), R(54) and R(55) identically or differently are hydrogen,(C₁-C₆)-alkyl; or R(69) and R(70), or R(54) and R(55) together with thecarbon atom carrying them are a (C₃-C₈)-cycloalkyl; R(63) is H,(C₁-C₆)-alkyl, (C₃-C₈)-cycloalkyl or —C_(e)H_(2e)—R(73); e is zero, 1,2, 3 or 4; R(56), R(57) and R(73) independently are phenyl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(74)R(75); R(74) andR(75)  are H or (C₁-C₄)-alkyl; or R(56), R(57) and R(73) independentlyare (C₁-C₉)-heteroaryl, which is unsubstituted or substitued as phenyl;R(58), R(59), R(60), R(61) and R(62) are hydrogen or methyl, or R(3) andR(4) independently of one another are R(76)—NH—SO₂—; R(76) isR(77)R(78)N—(C═Y′)—; Y′ is oxygen, S or N—R(79); R(77) and R(78)identically or differently are H, (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl,—C_(f)H_(2f)—R(80); f is zero, 1, 2, 3 or 4; R(80) is (C₅-C₇)-cycloalkylor phenyl, which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methoxy and(C₁-C₄)-alkyl; or R(77) and R(78) together are 4 or 5 methylene groups,of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃ orN-benzyl, R(79) is defined as R(77) or is amidine; or R(3) and R(4)independently of one another are NR(84)R(85); R(84) and R(85)independently of one another are H, (C₁-C₄)-alkyl, or together are 4 or5 methylene groups, of which one CH₂ group can be replaced by oxygen, S,NH, N—CH₃ or N-benzyl, or a pharmaceutically tolerable salt thereof; y)a bicyclic heteroaroylguanidine of the formula

in which: T, U, V, W, X, Y and Z independently of one another arenitrogen or carbon; but with the restriction that X and Z are notsimultaneously nitrogen, and that T, U, V, W, X, Y and Z carry nosubstituents if they are nitrogen, and that no more than four of themare simultaneously nitrogen, R(1) and R(2) independently of one anotherare hydrogen, F, Cl, Br, I, (C₁-C₃)-alkyl, (C₁-C₃)-perfluoroalkyl,OR(8), NR(8)R(9) or C(═O)N═C(NH₂)₂; R(8) and R(9) independently of oneanother are hydrogen or (C₁-C₃)-alkyl, or R(8) and R(9) together are 4or 5 methylene groups, of which one CH₂ group can be replaced by oxygen,S, NH, N—CH₃ or N-benzyl; R(3), R(4), R(5), R(6) and R(7) independentlyof one another are hydrogen, F, Cl, Br, I, —C≡N,X_(k)—(CH₂)_(p)—(C_(q)F_(2q+1)), R(10a)—SO_(bm), R(10b)R(10c)N—CO,R(11)—CO— or R(12)R(13)N—SO₂—, where the perfluoroalkyl group isstraight-chain or branched; X is oxygen, S or NR(14); R(14) is H or(C₁-C₃)-alkyl; bm is zero, 1 or 2; p is zero, 1 or 2; k is zero or 1; q1, 2, 3, 4, 5 or 6; R(10a), R(10b), R(11) and R(12) independently of oneanother are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, —C_(n)H_(2n)—R(15) or(C₁-C₈)-perfluoroalkyl; n is zero, 1, 2, 3 or 4; R(15) is(C₃-C₇)-cycloalkyl or phenyl, which is not substituted or is substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(16)R(17); R(16) and R(17)  are H or C₁-C₄-alkyl;or R(10b), R(11) and R(12) are hydrogen; R(10c) and R(13) independentlyare hydrogen or (C₁-C₄)-alkyl; or R(10b) and R(10c) and R(12) and R(13)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl; or R(3), R(4), R(5),R(6) and R(7) independently of one another are (C₁-C₉)-alkyl,—C_(al)H_(2al)R(18) or (C₃-C₈)-alkenyl; al is zero, 1 or 2; R(18) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(19a)R(19b);R(19a) and R(19b) are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;or R(3), R(4), R(5), R(6) and R(7) independently of one another are(C₁-C₉)-heteroaryl, which is linked via C or N and which isunsubstituted or substituted by 1-3 substituents from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; or R(3), R(4), R(5), R(6) and R(7) independently of oneanother are

Y is oxygen, —S— or —NR(22)—; h, ad, ah independently of one another arezero or 1; i, j, k, ae, af, ag, ao, ap and ak independently of oneanother are zero, 1, 2, 3 or 4; but where in each case h, i and k arenot simultaneously zero, ad, ae and ag are not simultaneously zero, andah, ao and ak are not simultaneously zero, R(23), R(24), R(25) and R(22)independently of one another are hydrogen or (C₁-C₃)-alkyl; or R(3),R(4), R(5), R(6) and R(7) independently of one another are SR(29),—OR(30), —NR(31)R(32) or —CR(33)R(34)R(35); R(29), R(30), R(31) andR(33) independently of one another are —C_(a)H_(2a)—(C₁-C₉)-heteroaryl,which is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; a is zero, 1 or 2; R(32), R(34) and R(35)independently of one another are defined as R(29) or are hydrogen,(C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; or R(3), R(4), R(5), R(6) andR(7) independently of one another are

R(96), R(97) and R(98) independently of one another are(C₁-C₉)-heteroaryl, which is linked via C or N and which is unsubstituedor substituted by 1 to 3 substituents from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino, dimethylamino andbenzyl; W is oxygen, S or NR(36)—; R(36) is H or (C₁-C₄)-alkyl; or R(3),R(4), R(5), R(6) and R(7) independently of one another are R(46)X(1)—;X(1) is oxygen, S, NR(47), (D═O)A— or NR(48)C═MN^((*))R(49)—; M isoxygen or sulfur; A is oxygen or NR(50); D is C or SO; R(46) is(C₁-C₈)-alkyl, (C₃-C₈)-alkenyl, (CH₂)_(b)C_(d)F_(2d+1) or—C_(x)H_(2x)—R(51); b is zero or 1; d is 1, 2, 3, 4, 5, 6 or 7; x iszero, 1, 2, 3 or 4; R(51) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl ornaphthyl, where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(52)R(53); R(52) and R(53)  are hydrogen,(C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(47), R(48) and R(50)independently are hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl;R(49) is defined as R(46); or R(46) and R(47), or R(46) and R(48)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;  where A and N^((*))are bonded to the phenyl nucleus of the heteroaroylguanidine parentstructure; or R(3), R(4), R(5), R(6) and R(7) independently of oneanother are —SR(64), —OR(65), —NHR(66), —NR(67)R(68), —CHR(69)R(70) or—CR(54)R(55)OH, —C≡CR(56), —CR(58)═CR(57) or—[CR(59)R(60)]_(u)—CO—[CR(61)R(62)]_(v)—R(63); R(64), R(65), R(66),R(67) and R(69) identically or differently are—(CH₂)_(y)—(CHOH)_(z)—(CH₂)_(aa)—(CHOH)_(t)—R(71) or—(CH₂)_(ab)—O—(CH₂—CH₂O)_(ac)—R(72); R(71) and R(72) independently ofone another are hydrogen or methyl; u is 1, 2, 3 or 4; v is zero, 1, 2,3 or 4; y, z, aa, ab and ac identically or differently are zero, 1, 2, 3or 4; t is 1, 2, 3 or 4; R(68), R(70), R(54) and R(55) identically ordifferently are hydrogen or (C₁-C₆)-alkyl; or R(69) and R(70), or R(54)and R(55) together with the carbon atom carrying them are(C₃-C₈)-cycloalkyl; R(63) is hydrogen, (C₁-C₆)-alkyl, (C₃-C₈)-cycloalkylor —C_(e)H_(2e)—R(73); e is zero, 1, 2, 3 or 4; R(56), R(57) and R(73)independently are phenyl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(74)R(75); R(74) and R(75) are hydrogen or (C₁-C₄)-alkyl;or R(56), R(57) and R(73) independently are (C₁-C₉)-heteroaryl, which isunsubstituted or substituted as phenyl; R(58), R(59), R(60), R(61) andR(62) are hydrogen or methyl; or R(3), R(4), R(5), R(6) and R(7)independently of one another are R(76)—NH—SO₂—; R(76) isR(77)R(78)N—(C═Y′)—; Y′ is oxygen, S or N—R(79); R(77) and R(78)identically or differently are hydrogen, (C₁-C₈)-alkyl, (C₃-C₆)-alkenylor —C_(f)H_(2f)R(80); f is zero, 1, 2, 3 or 4; R(80) is(C₅-C₇)-cycloalkyl or phenyl, which is  unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methoxy and (C₁-C₄)-alkyl; or R(77) and R(78) together are 4 or 5methylene groups, of which one CH₂ group can be replaced by oxygen,sulfur, NH, N—CH₃ or N-benzyl; R(79) is defined as R(77) or is amidine;or R(3), R(4), R(5), R(6) and R(7) independently of one another areNR(84a)R(85), OR(84b), SR(84c) or —C_(n)H_(2n)—R(84d); n is zero, 1, 2,3 or 4; R(84d) is (C₃-C₇)-cycloalkyl or phenyl, which is not substitutedor is substituted by 1-3 substituents from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(16)R(17); R(16) and R(17) are hydrogen,or C₁-C₄-alkyl; R(84a), R(84b), R(84c) and R(85) independently of oneanother are hydrogen, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl or(CH₂)_(ax)—R(84g); ax is zero, 1, 2, 3 or 4; R(84g) is(C₃-C₇)-cycloalkyl or phenyl, which is not substituted or is substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(84u)R(84v); R(84u) and R(84v)  are hydrogen orC₁-C₄-alkyl; or R(84a) and R(85) together are 4 or 5 methylene groups,of which one CH₂ group can be replaced by oxygen, sulfur, NH, N—CH₃ orN-benzyl, or a pharmaceutically tolerable salt thereof; z) abenzoylguanidine of the formula

in which: R(1) is R(6)—SO_(m); m is zero, 1 or 2; R(6) is perfluoroalkylhaving 1, 2, 3, 4, 5 or 6 carbon atoms, which is straight-chain orbranched; R(2) and R(3) independently of one another are hydrogen, F,Cl, Br, I, alkyl having 1, 2, 3 or 4 carbon atoms, alkoxy having 1, 2, 3or 4 carbon atoms or phenoxy, which is unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, methyl andmethoxy; or R(2) and R(3) independently of one another are pyrrol-1-yl,pyrrol-2-yl- or pyrrol-3-yl, which is not substituted or is substitutedby 1 to 4 substituents selected from the group consisting of F, Cl, Br,I, CN, alkanoyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkoxycarbonyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms, formyl,carboxyl, CF₃, methyl and methoxy; R(4) and R(5) independently of oneanother are hydrogen, alkyl having 1, 2 or 3 carbon atoms, F, Cl, Br, I,CN, OR(7), NR(8)R(9) or —(CH₂)_(n)—(CF₂)_(o)—CF₃; R(7), R(8) and R(9)independently of one another are hydrogen or alkyl having 1, 2, 3 or 4carbon atoms; n is zero or 1; o is zero, 1 or 2; or a pharmacologicallyacceptable salt thereof; ab) a phenyl-substituted alkenylcarboxylic acidguanidide of the formula

in which: R(A) is hydrogen, F, Cl, Br, I, CN, OH, OR(6), (C₁-C₈)-alkyl,O_(r)(CH₂)_(a)C_(b)F_(2b+1), (C₃-C₈)-cycloalkyl or NR(7)R(8); r is zeroor 1; a is zero, 1, 2, 3 or 4; b is 1, 2, 3, 4, 5, 6, 7 or 8; R(6) is(C₁-C₈)-alkyl, (C₁-C₄)-perfluoroalkyl, (C₃-C₈)-alkenyl,(C₃-C₈)-cycloalkyl, phenyl or benzyl; where the aromatics are notsubstituted or are substituted by 1-3 substituents from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(9)R(10); R(9) and R(10)are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(7) and R(8)independently of one another are defined as R(6); or R(7) and R(8)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl; R(B) independently isdefined as R(A); X is zero, 1 or 2; Y is zero, 1 or 2; R(C) is hydrogen,F, Cl, Br, I, CN, OR(12), (C₁-C₈)-alkyl, O_(p)(CH₂)_(f)C_(g)F_(2g+1) or(C₃-C₈)-cycloalkyl; p is zero or 1; f is zero, 1, 2, 3 or 4; g is 1, 2,3, 4, 5, 6, 7 or 8; R(12) is (C₁-C₈)-alkyl, (C₁-C₄)-perfluoroalkyl,(C₃-C₈)-alkenyl, (C₃-C₈)-cycloalkyl, phenyl or benzyl; where thearomatics phenyl or benzyl are not substituted or are substituted by 1-3substituents from the group consisting of F, Cl, CF₃, methyl, methoxyand NR(13)R(14); R(13) and R(14)  independently of one another are H,(C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(D) independently is definedas R(C), R(1) is hydrogen, (C₁-C₈)-alkyl, —O_(t)(CH₂)_(d)C_(e)F_(2e+1),(C₃-C₈)-cycloalkyl, F, Cl, Br, I or CN; t is zero or 1; d is zero, 1, 2,3 or 4; e is 1, 2, 3, 4, 5, 6, 7 or 8; R(2), R(3), R(4) and R(5)independently of one another are defined as R(1); but with the conditionthat at least one of the substituents R(A), R(B), R(C), R(D), R(1),R(2), R(4) or R(5) is an O_(r)(CH₂)_(a)C_(b)F_(2b+1),O_(p)(CH₂)_(f)C_(g)F_(2g+1) or O_(t)(CH₂)_(d)C_(e)F_(2e+1) group andR(3) is not an O_(t)(CH₂)_(d)C_(e)F_(2e+1) group; or pharmaceuticallytolerable salt thereof; ac) an ortho-amino-substituted benzoylguanidineof the formula

in which: R(1) is NR(50)R(6), R(50) and R(6) independently of oneanother are hydrogen, (C₁-C₈)-alkyl or (C₁-C₈)-perfluoroalkyl; R(2),R(3), R(4) and R(5) independently of one another are R(10)—SO_(a)—,R(11)R(12)N—CO—, R(13)—CO— or R(14)R(15)N—SO₂—; a is zero, 1 or 2,R(10), R(11), R(12), R(13), R(14) and R(15) independently of one anotherare (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₆)-alkenyl or—C_(ab)H_(2ab)—R(16); ab is zero, 1, 2, 3 or 4; R(16) is(C₃-C₇)-cycloalkyl, phenyl, which is not substituted or is substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy or NR(17)R(18); R(17) and R(18)  independently of oneanother are H, CF₃ or (C₁-C₄)-alkyl; or R(11), R(12), and also R(14) andR(15) together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, S, NH, N—CH₃ or N-benzyl; or R(11), R(12), R(14)and R(15) independently of one another are hydrogen; or R(2), R(3), R(4)and R(5) independently of one another are SR(21), —OR(22), —NR(23)R(24)or —CR(25)R(26)R(27); R(21), R(22), R(23) and R(25) independently of oneanother are —C_(b)H_(2b)—(C₁-C₉)-heteroaryl, which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; bis zero, 1 or 2; R(24), R(26) and R(27) independently of one another arehydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; or R(2), R(3), R(4)and R(5) independently of one another are hydrogen, F, Cl, Br, I, CN,—(Xa)_(dg)—C_(da)H_(2da+1), —(Xb)_(dh)—(CH₂)_(db)—C_(de)F_(2de+1),(C₃-C₈)-alkenyl or —C_(df)H_(2df)R(30); (Xa) is O, S or NR(33); R(33) isH, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; dg is zero or 1; (Xb) is O,S or NR(34); R(34) is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; dh iszero or 1; da is zero, 1, 2, 3, 4, 5, 6, 7, 8; db is zero, 1, 2, 3, 4;de is zero, 1, 2, 3, 4, 5, 6, 7; df is zero, 1, 2, 3, 4; R(30) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsphenyl, biphenylyl or naphthyl are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(31)R(32); R(31) and R(32) are H, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; or R(2), R(3), R(4) and R(5) independently ofone another are NR(40)R(41) or —(Xe)—(CH₂)_(eb)R(45); R(40) and R(41)independently of one another are hydrogen, (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl or (CH₂)_(e)—R(42); e is zero, 1, 2, 3 or 4;R(42) is (C₃-C₇)-cycloalkyl, phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(43)R(44); R(43) and R(44)  independentlyof one another are H, CF₃ or (C₁-C₄)-alkyl; or R(40) and R(41) togetherare 4 or 5 methylene groups, of which one CH₂ group can be replaced byoxygen, sulfur, NH, N—CH₃ or N-benzyl; (Xe) is O, S or NR(47); R(47)  isH, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; eb is zero, 1, 2, 3 or 4;R(45) is (C₃-C₇)-cycloalkyl, phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy, NR(50)R(51) and —(Xfa)—(CH₂)_(ed)—(Xfb)R(46);Xfa is CH₂, O S or NR(48); Xfb is O, S or NR(49); ed is 1, 2, 3 or 4;R(46)  is H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(48), R(49),R(50) and R(51)  independently of one another are H or (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; where R(3) and R(4), however, cannot behydrogen, or pharmaceutically tolerable salt thereof; ad) abenzoylguanidine of the formula

in which: one of the three substituents R(1), R(2) and R(3) is(C₁-C₉)-heteroaryl-N-oxide, which is linked via C or N and which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; or one of the three substituents R(1), R(2) and R(3) is—SR(10), —OR(10), —NR(10)R(11) or —CR(10)R(11)R(12); R(10) is—C_(a)H_(2a)(C₁-C₉)-heteroaryl-N-oxide, which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; ais zero, 1 or 2; R(11) and R(12) independently of one another aredefined as R(10), are hydrogen or (C₁-C₄)-alkyl; and the othersubstituents R(1), R(2) and R(3) in each case independently of oneanother are (C₁-C₈)-alkyl, (C₂-C₈)-alkenyl or —C_(m)H_(2m)R(14); m iszero, 1 or 2; R(14) is (C₃-C₈)-cycloalkyl or phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(15)R(16), R(15)and R(16)  are hydrogen or CH₃; or the other substituents R(1), R(2) andR(3) in each case independently of one another are hydrogen, F, Cl, Br,I, —C≡N, X—(CH₂)_(p)—(C_(q)F_(2q+1)), R(22)—SO_(u), R(23)R(24)N—CO,R(25)—CO— or R(26)R(27)N—SO₂—, where the perfluoroalkyl group isstraight-chain or branched; X is a bond, oxygen, S or NR(28); u is zero,1 or 2; p is zero, 1 or 2; q is zero, 1, 2, 3, 4, 5 or 6; R(22), R(23),R(25) and R(26) independently are (C₁-C₈)-alkyl, (C₂-C₆)-alkenyl,—C_(n)H_(2n)—R(29) or CF₃; n is zero, 1, 2, 3 or 4; R(28) is hydrogen or(C₁-C₃)-alkyl; R(29) is (C₃-C₇)-cycloalkyl or phenyl; which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(30)R(31); R(30)and R(31)  are hydrogen or C₁-C₄-alkyl, or R(23), R(25) and R(26) arealso hydrogen; R(24) and R(27) independently of one another are hydrogenor (C₁-C₄)-alkyl; or R(23) and R(24), and also R(26) and R(27) togetherare 4 or 5 methylene groups, of which one CH₂ group can be replaced byoxygen, S, NH, N—CH₃ or N-benzyl; or the other substituents R(1), R(2)and R(3) in each case independently of one another are OR(35) orNR(35)R(36); R(35) and R(36) independently of one another are hydrogenor (C₁-C₆)-alkyl; or R(35) and R(36) together are 4-7 methylene groups,of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃ orN-benzyl, R(4) and R(5) independently of one another are hydrogen,(C₁-C₄)-alkyl, F, Cl, —OR(32), —NR(33)R(34) or C_(r)F_(2r+1); R(32),R(33) and R(34) independently of one another are hydrogen or(C₁-C₃)-alkyl; r is 1, 2, 3 or 4; or pharmaceutically tolerable saltthereof; ae) a benzoylguanidine of the formula

in which: R(1) is hydrogen, F, Cl, Br, I, CN, NO₂, OH, (C₁-C₈)-alkyl,(C₃-C₈)-cycloalkyl or O_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃; a is zero or 1; bis zero, 1 or 2; c is zero, 1, 2 or 3; or R(1) is R(5)—SO_(m) orR(6)R(7)N—SO₂—; m is zero, 1 or 2; R(5) and R(6) independently of oneanother are (C₁-C₈)-alkyl, (C₃-C₆)-alkenyl, CF₃ or —C_(n)H_(2n)—R(8); nis zero, 1, 2, 3 or 4; R(7) is hydrogen or (C₁-C₄)-alkyl; R(8) is(C₃-C₇)-cycloalkyl or phenyl, which is not substituted or is substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(9)R(10); R(9) and R(10) independently of oneanother are hydrogen or (C₁-C₄)-alkyl; or R(6) is H; or R(6) and R(7)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl, or R(1) is —SR(11),—OR(11) or —CR(11)R(12)R(13); R(11) is —C_(p)C_(p)H_(2p)—(C₃-C₈)-cycloalkyl, —(C₁-C₉)-heteroaryl or phenyl, where the aromaticsystems are unsubstituted or substituted by 1-3 substituents selectedfrom the group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; R(12), R(13) independently of one anotherare defined as R(11) or are hydrogen or (C₁-C₄)-alkyl; p is zero, 1 or2; or R(1) is phenyl, naphthyl, biphenylyl or (C₁-C₉)-heteroaryl, thelatter linked via C or N, which are unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; R(2) is—CF₂R(14), —CF[R(15)][R(16)], —CF[(CF₂)_(q)—CF₃)][R(15)] or—C[(CF₂)_(r)—CF₃]═CR(15)R(16); R(14) is (C₁-C₄)-alkyl or(C₃-C₆)-cycloalkyl; R(15) and R(16) independently of one another arehydrogen or (C₁-C₄)-alkyl; q is zero, 1 or 2; r is zero, 1 or 2; R(3) isdefined as R(1); R(4) is hydrogen, (C₁-C₃)-alkyl, F, Cl, Br, I, CN or—(CH₂)_(s)—(CF₂)_(t)—CF₃; s is zero or 1; t is zero, 1 or 2; orpharmaceutically tolerable salt thereof; af) a benzoylguanidine of theformula

in which: one of the three substituents R(1), R(2) and R(3) is—Y-4-[(CH₂)_(k)—CHR(7)—(C═O)R(8)]-phenyl,—Y-3—(CH₂)_(k)—CHR(7)—(C═O)R(8)]-phenyl or—Y-2-[(CH₂)_(k)—CHR(7)—(C═O)R(8)]-phenyl, where the phenyl in each caseis unsubstituted or substituted by 1-2 substituents from the group F,Cl, —CF₃, methyl, hydroxyl, methoxy, and —NR(37)R(38); R(37) and R(38)independently of one another are hydrogen or —CH₃; Y is a bond, oxygen,—S— or —NR(9); R(9) is hydrogen or —(C₁-C₄)-alkyl; R(7) is —OR(10) or—NR(10)R(11); R(10) and R(11) independently of one another are hydrogen,—(C₁-C₈)-alkyl, —(C₁-C₈)-alkanoyl, —(C₁-C₈)-alkoxycarbonyl, benzyl,benzyloxycarbonyl; or R(10) is trityl; R(8) is —OR(12) or —NR(12)R(13);R(12) and R(13) independently of one another are hydrogen,—(C₁-C₈)-alkyl or benzyl; k is zero, 1, 2, 3 or 4; and the otherradicals R(1), R(2) and R(3) in each case independently of one anotherare —(C₁-C₈)-alkyl, —(C₂-C₈)-alkenyl or —(CH₂)_(m)R(14); m is zero, 1 or2; R(14) is —(C₃-C₈)-cycloalkyl or phenyl, which is not substituted oris substituted by 1-3 substituents selected from the group consisting ofF, Cl, —CF₃, methyl, methoxy and —NR(15)R(16); R(15) and R(16) arehydrogen or —CH₃; or the other radicals R(1), R(2) and R(3) in each caseindependently of one another are R(18)R(19)N—(C═Y′)—NH—SO₂—; Y′ isoxygen, —S— or —N—R(20); R(18) and R(19) independently of one anotherare hydrogen, —(C₁-C₈)-alkyl, —(C₃-C₆)-alkenyl or —(CH₂)_(t)—R(21); t iszero, 1, 2, 3 or 4; R(21) is —(C₅-C₇)-cycloalkyl or phenyl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, —CF₃, methoxy and —(C₁-C₄)-alkyl; or R(18) andR(19) together are 4 or 5 methylene groups, of which one CH₂ group canbe replaced by oxygen, —S—, —NH—, —N—CH₃ or —N-benzyl; R(20) is definedas R(18) or is amidine; or the other radicals R(1), R(2) and R(3) ineach case independently of one another are hydrogen, F, Cl, Br, I, —C≡N,X—(CH₂)_(p)—(C_(q)F_(2q+1)), R(22)—SO_(u)—, R(23)R(24)N—CO—, R(25)—CO—or R(26)R(27)N—SO₂—, where the perfluoroalkyl group is straight-chain orbranched; X is a bond, oxygen, —S— or —NR(28); u is zero, 1 or 2; p iszero, 1 or 2; q is 1, 2, 3, 4, 5 or 6; R(22), R(23), R(25) and R(26)independently of one another are —(C₁-C₈)-alkyl, —(C₃-C₆)-alkenyl,—(CH₂)_(n)—R(29) or —CF₃; n is zero, 1, 2, 3 or 4; R(28) is hydrogen or—(C₁-C₃)-alkyl; R(29) is —(C₃-C₇)-cycloalkyl or phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, —CF₃, methyl, methoxy and —NR(30)R(31); R(30)and R(31)  are hydrogen or —(C₁-C₄)-alkyl; or R(23), R(25) and R(26) arehydrogen; R(24) and R(27) independently of one another are hydrogen or—(C₁-C₄)-alkyl; or R(23) and R(24), and also R(26) and R(27) togetherare 4 or 5 methylene groups, of which one CH₂ group can be replaced byoxygen, —S—, —NH—, —N—CH₃ or —N-benzyl; or the other radicals R(1), R(2)and R(3) in each case independently of one another are —OR(35) or—NR(35)R(36); R(35) and R(36) independently of one another are hydrogenor —(C₁-C₆)-alkyl; or R(35) and R(36) together are 4-7 methylene groups,of which one CH₂ group can be replaced by oxygen, —S—, —NH—, —N—CH₃ or—N-benzyl; R(4) and R(5) independently of one another are hydrogen,—(C₁-C₄)-alkyl, F, Cl, —OR(32), —NR(33)R(34) or —C_(r)F_(2r+1); R(32),R(33) and R(34) independently of one another are hydrogen or—(C₁-C₃)-alkyl; r is 1, 2, 3 or 4; or pharmaceutically tolerable saltthereof; ag) a benzoylguanidine of the formula

in which: R(1) is R(6)—CO or R(7)R(8)N—CO; R(6) is (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or —C_(n)H_(2n)—R(9), n is zero,1, 2, 3 or 4; R(9) is (C₃-C₉)-cycloalkyl, phenyl, biphenylyl ornaphthyl, where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(10)R(11), R(10) and R(11)  are H, (C₁-C₄)-alkylor (C₁-C₄)-perfluoroalkyl; R(7) is H, (C₁-C₈)-alkyl,(C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or —C_(n)H_(2n)—R(12); n iszero, 1, 2, 3 or 4; R(12) is (C₃-C₈)-cycloalkyl, phenyl, biphenylyl ornaphthyl, where the aromatics are not substituted or are substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(13)R(14); R(13) and R(14)  are H, (C₁-C₄)-alkylor (C₁-C₄)-perfluoroalkyl; R(8) is H, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; or R(7) and R(8) together are 4 or 5 methylenegroups, of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃or N-benzyl; R(2) is defined as R(1), or is H, OH, F, Cl, Br, I, CN,NO₂, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(n)H_(2n)R(15); n is zero, 1, 2, 3 or 4; R(15) is (C₃-C₈)-cycloalkyl,phenyl, biphenylyl or naphthyl, where the aromatics are not substitutedor are substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, methyl, methoxy and NR(16)R(17); R(16) andR(17) are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; or R(2) is(C₁-C₉)-heteroaryl, which is linked via C or N and which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; or R(2) is SR(18), —OR(18), —NR(18)R(19) or—CR(18)R(19)R(20); R(18) is —C_(a)H_(2a)—(C₁-C₉)-heteroaryl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino,and dimethylamino; a is zero, 1 or 2; R(19) and R(20) independently ofone another are defined as R(18) or are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; or R(2) is R(21)—SO_(m) or R(22)R(23)N—SO₂—; mis 1 or 2; R(21) is (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl,(C₃-C₈)-alkenyl or —C_(n)H_(2n)—R(24); n is zero, 1, 2, 3 or 4; R(24) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(27)R(28);R(27) and R(28)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(22)is H, (C₁-C₈)-alkyl, (C₁-C₈)-perfluoroalkyl, (C₃-C₈)-alkenyl or—C_(n)H_(2n)—R(29); n is zero, 1, 2, 3 or 4; R(29) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(30)R(31);R(30) and R(31)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(23)is hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; or R(22) and R(23)together are 4 or 5 methylene groups, of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl; or R(2) is R(33)X—; X isoxygen, S, NR(34), (D═O)A— or NR(34)C═MN^((*))R(35)—; M is oxygen or S;A is oxygen or NR(34); D is C or SO; R(33) is (C₁-C₈)-alkyl,(C₃-C₈)-alkenyl, (CH₂)_(b)C_(d)F_(2d+1) or —C_(n)H_(2n)—R(36); b is zeroor 1; d is 1, 2, 3, 4, 5, 6 or 7; n is zero, 1, 2, 3, or 4; R(36) is(C₃-C₈)-cycloalkyl, phenyl, biphenylyl or naphthyl,  where the aromaticsare not substituted or are substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy and NR(37)R(38); R(37) and R(38)  are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(34)is hydrogen, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; R(35) is definedas R(33); or R(33) and R(34) together are 4 or 5 methylene groups, ofwhich one CH₂ group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl; where A and N^((*)) are bonded to the phenyl nucleus of thebenzoylguanidine parent structure; or R(2) is —SR(40), —OR(40),—NHR(40), —NR(40)R(41), —CHR(40)R(42), —CR(42)R(43)OH, —C≡CR(45),—CR(46)═CR(45) or —[CR(47)R(48)]_(u)—CO—[C(R49)R(50)]_(v)—R(44); R(40)and R(41) independently of one another are—(CH₂)_(p)—(CHOH)_(q)—(CH₂)_(r)—(CHOH)_(t)—R(51) or—(CH₂)_(p)—O—(CH₂—CH₂O)_(q)—R(51); R(51) is hydrogen or methyl; u is 1,2, 3 or 4; v is zero, 1, 2, 3 or 4; p, q and r independently of oneanother are zero, 1, 2, 3 or 4; t is 1, 2, 3 or 4; R(42) and R(43)independently of one another are hydrogen or (C₁-C₆)-alkyl; or R(42) andR(43) together with the carbon atom carrying them are a(C₃-C₈)-cycloalkyl; R(44) is hydrogen, (C₁-C₆)-alkyl,(C₃-C₈)-cycloalkyl, —C_(e)H_(2e)—R(45); e is zero, 1, 2, 3 or 4; R(45)is phenyl, which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(52)R(53); R(52) and R(53) are H or (C₁-C₄)-alkyl; or R(45) is(C₁-C₉)-heteroaryl, which is unsubstituted or substituted as phenyl; orR(45) is (C₁-C₆)-alkyl, which is unsubstituted or substituted by 1-3 OH;R(46), R(47), R(48), R(49) and R(50) independently of one another arehydrogen or methyl; or R(2) is R(55)—NH—SO₂—; R(55) isR(56)R(57)N—(C═Y)—; Y is oxygen, S or N—R(58); R(56) and R(57)independently of one another are hydrogen, (C₁-C₈)-alkyl,(C₃-C₆)-alkenyl or —C_(f)H_(2f)—R(59); f is zero, 1, 2, 3 or 4; R(59) is(C₅-C₇)-cycloalkyl or phenyl, which is unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methoxy and (C₁-C₄)-alkyl; or R(56) and R(57) together are 4 or 5methylene groups, of which one CH₂ group can be replaced by oxygen, S,NH, N—CH₃ or N-benzyl; R(58) is defined as R(56) or is amidine; R(3),R(4) and R(5) are independently of one another defined as R(1) or R(2),but where at least one of the substituents R(2), R(3), R(4) and R(5)must be OH; or pharmaceutically tolerable salt thereof; ah) abenzoylguanidine of the formula

in which: one of the three substituents R(1), R(2) and R(3) isR(6)—A-B-D-; R(6) is an amino group —NR(7)R(8), an amidino groupR(7)R(8)N—C[═N—R(9)]— or a guanidino group

R(7), R(8), R(9) and R(10) independently of one another are hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms; or R(7) and R(8) together areC_(a)H_(2a); a is 4, 5,6 or 7; where if a=5, 6 or 7 a methylene group ofthe group C_(a)H_(2a) can be replaced by a heteroatom group O, SO_(m) orNR(11), or R(8) and R(9) or R(9) and R(10) or R(7) and R(10) are a groupC_(a)H_(2a); a is 2, 3, 4 or 5;  where if a=3, 4 or 5 a methylene groupof the group C_(a)H_(2a) can be replaced by a heteroatom group O, SO_(m)or NR(11); m is zero, 1 or 2; R(11) is hydrogen or methyl; or R(6) is abasic heteroaromatic ring system having 1-9 carbon atoms; A isC_(b)H_(2b); b is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; where in the groupC_(b)H_(2b) one or two methylene groups can be replaced by one of thegroupings selected from the group consisting of —O—, —CO—, —CH[OR(20)]—,—SO_(m)—, —NR(20)—, —NR(20)—CO—, —NR(20)—CO—NH—, —NR(20)—CO—NH—SO₂—

 and —SO_(aa)[NR(19)]_(bb)—;  and where in the group C_(b)H_(2b) amethylene group can be replaced by —CH—R(99), where R(99) together withR(7) forms a pyrrolidine or piperidine ring;  aa is 1 or 2;  bb is 0 or1;  aa+bb=2;  R(19) is hydrogen or alkyl having 1, 2, 3 or 4 carbonatoms;  R(20) is hydrogen or methyl; B is a phenylene or naphthyleneradical

R(12) and R(13) independently of one another are hydrogen, methyl, F,Cl, Br, I, CF₃ or —SO_(w)—R(14); R(14) is methyl or NR(15)R(16); R(15)and R(16)  independently of one another are hydrogen or alkyl having 1,2, 3 or 4 carbon atoms; w is zero, 1 or 2; D is —C_(d)H_(2d)—X_(f)—; dis zero, 1, 2, 3 or 4; X is —O—, —CO—, —CH[OR(21)]—, —SO_(m)— or—NR(21)—; f is zero or 1; R(21) is hydrogen or methyl; m is zero, 1 or2; and the other substituents R(1) and R(2) and R(3) in each caseindependently of one another are hydrogen, F, Cl, Br, I, —CN,—(C₁-C₈)-alkyl, —(C₂-C₈)-alkenyl, —NR(35)R(36) orR(17)—C_(g)H_(2g)—Z_(h)—; g is zero, 1, 2, 3 or 4; h is zero or 1; R(35)and R(36) independently of one another are hydrogen or alkyl having 1,2, 3, 4, 5 or 6 carbon atoms; or R(35) and R(36) together are 4-7methylene groups, of which one CH₂ group can be replaced by oxygen, —S—,—NH—, —NCH₃ or —N-benzyl; Z is —O—, —CO—, —SO_(v)—, —NR(18)—,—NR(18)—CO—, —NR(18)—CO—NH— or —NR(18)—SO₂—; R(18) is hydrogen ormethyl; v is zero, 1 or 2; R(17) is hydrogen, cycloalkyl having 3, 5 or6 carbon atoms or C_(k)F_(2k+1)—; k is 1, 2 or 3, or R(17) ispyrrol-1-yl, pyrrol-2-yl or pyrrol-3-yl, which is not substituted or issubstituted by 1-4 substituents selected from the group consisting of F,Cl, Br, I, —CN, (C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl,carboxyl, —CF₃, methyl and methoxy; or R(17) —is (C₃-C₈)-cycloalkyl orphenyl, which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, hydroxyl,methoxy, —NR(37)R(38), CH₃SO₂— and H₂NO₂S—; R(37) and R(38) are hydrogenor —CH₃; R(4) and R(5) independently of one another are hydrogen, alkylhaving 1, 2, 3 or 4 carbon atoms, F, Cl, —OR(32), —NR(33)R(34) or—C_(r)F_(2r+1); R(32), R(33) and R(34) independently of one another arehydrogen or alkyl having 1, 2 or 3 carbon atoms; r is 1, 2, 3 or 4; orpharmacologically tolerable salt thereof; ai) an indenoylguanidine ofthe formula

in which: R(1) and R(2) independently of one another are hydrogen, alkylhaving 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms, cycloalkyl having3, 4, 5 or 6 carbon atoms, O-alkyl having 1, 2, 3 or 4 carbon atoms,O—C(═O)-alkyl having 1, 2, 3 or 4 carbon atoms orC_(m)H_(2m)—NR(12)R(13); R(12) and R(13) independently of one anotherare hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; m is zero, 1, 2,3 or 4; or R(1) and R(2) independently of one another are NH—C(═O)—NH₂,C(═O)—O—alkyl having 1, 2, 3 or 4 carbon atoms, C(═O)—NH₂,C(═O)—NH-alkyl having 1, 2, 3 or 4 carbon atoms, C(═O)—N(alkyl)₂ having1, 2, 3 or 4 carbon atoms in each alkyl group, alkenyl having 2, 3, 4,5, 6, 7, 8, 9 or 10 carbon atoms, alkynyl having 2, 3, 4, 5, 6, 7, 8, 9or 10 carbon atoms, alkylaryl having 1, 2, 3 or 4 carbon atoms in thealkyl group, alkenylaryl having 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbonatoms in the alkenyl group, alkynylaryl having 2, 3, 4, 5, 6, 7, 8, 9 or10 carbon atoms in the alkynyl group, C₁-C₄-alkyl-substituted aryl,C₁-C₄-alkylheteroaryl, C₁-C₄-alkenylheteroaryl, aminoalkylaryl having 1,2, 3 or 4 carbon atoms in the alkyl group, substituted aryl, heteroaryland substituted heteroaryl; R(3), R(4), R(5) and R(6) independently ofone another are hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10carbon atoms, O-alkyl having 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbonatoms, halogen, OH, aryl, substituted aryl, heteroaryl, substitutedheteroaryl, O-lower alkyl, O-aryl, O-lower alkylaryl, O-substitutedaryl, O-lower alkyl-substituted aryl, O—C(═O)—C₁-C₄-alkylaryl,O—C(═O)—NH—C₁-C₄-alkyl, O—C(═O)—N(C₁-C₄-alkyl)₂, NO₂, CN, CF₃, NH₂,NH—C(═O)—C₁-C₄-alkyl, NH—C(═O)—NH₂, COOH, C(═O)—O—C₁-C₄-alkyl,C(═O)—NH₂, C(═O)—NH—C₁-C₄-alkyl, C(═O)—N(C₁—C₄-alkyl)₂, C₁-C₄—COOH,C₁-C₄-alkyl-C(═O)—O—C₁-C₄-alkyl, SO₃H, SO₂-alkyl, SO₂-alkylaryl,SO₂—N-(alkyl)₂, SO₂—N(alkyl)(alkylaryl), C(═O)—R(11),C₁-C₁₀-alkyl-C(═O)—R(11), C₂-C₁₀-alkenyl-C(═O)—R(11),C₂-C₁₀-alkynyl-C(═O)—R(11), NH—C(═O)—C₁-C₁₀-alkyl-C(═O)—R(11) orO—C₁-C₄-alkyl-C(═O)—R(11); R(11) is C₁-C₄-alkyl, C₁-C₄-alkynyl, aryl,substituted aryl, NH₂, NH—C₁-C₄-alkyl, N—(C₁-C₄-alkyl)₂, SO₃H,SO₂-alkyl, SO₂-alkylaryl, SO₂—N-(alkyl)₂ or SO₂—N(alkyl)(alkylaryl); Xis O, S or NH; R(7), R(8), R(9) and R(10) independently of one anotherare hydrogen, alkyl, cycloalkyl, aryl, alkylaryl; or R(8) and R(9)together are part of a 5-, 6- or 7-membered heterocyclic ring; A isabsent or is a nontoxic organic or inorganic acid; ak) abenzyloxycarbonylguanidine of the formula

in which: R(1), R(2) and R(3) independently of one another are—Y-[4—R(8)-phenyl], —Y-[3—R(8)-phenyl] or —Y-[2—R(8)-phenyl], where thephenyl is in each case unsubstituted or substituted by 1-2 substituentsfrom the group consisting of F, Cl, —CF₃, methyl, hydroxyl, methoxy and—NR(96)R(97); R(96) and R(97) independently of one another are hydrogenor —CH₃; Y is a bond, CH₂, oxygen, —S— or —NR(9); R(9) is hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms; R(8) isSO_(a)[NR(98)]_(b)NR(99)R(10); a is 1 or 2; b is 0 or 1; a+b=2; R(98),R(99) and R(10) independently of one another are hydrogen,—(C₁-C₈)-alkyl, benzyl, —(C₂-C₈)-alkylene-NR(11)R(12),(C₂-C₈)-alkylene-NR(13)—(C₂-C₈)-alkylene-NR(37)R(38) or(C₀-C₈)-alkylene-CR(39)R(40)CR(41)R(42)(C₀-C₈)-alkylene-NR(43)R(44);R(11), R(12), R(13), R(37), R(38), R(43) and R(44)  independently of oneanother are hydrogen, —(C₁-C₈)-alkyl or benzyl; R(39), R(40), R(41) andR(42)  independently of one another are hydrogen, —(C₁-C₈)-alkyl or—(C₀-C₃)-alkylenephenyl,  where the phenyl is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, —CF₃, methyl and methoxy; or R(99) and R(10) together are 4-6methylene groups, of which one CH₂ group can be replaced by oxygen, —S—,—NH—, —N—CH₃ or —N-benzyl; or R(8) isSO_(a)[NR(98)]_(b)NR(95)—C[═N—R(94)]—NR(93)R(92); R(92), R(93), R(94)and R(95) independently of one another are hydrogen or alkyl having 1,2, 3 or 4 carbon atoms; or R(1), R(2) and R(3) independently of oneanother are pyrrol-1-yl, pyrrol-2-yl or pyrrol-3-yl, which is notsubstituted or is substituted by 1-4 substituents selected from thegroup consisting of F, Cl, Br, I, —CN, (C₂-C₈)-alkanoyl,(C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃, methyl, and methoxy; orR(1), R(2) and R(3) independently of one another are hydrogen,—(C₁-C₈)-alkyl, —(C₂-C₈)-alkenyl or —(CH₂)_(m)R(14); m is zero, 1 or 2;R(14) is —(C₃-C₈)-cycloalkyl or phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of Fand Cl, —CF₃, methyl, methoxy and —NR(15)R(16); R(15) and R(16) arehydrogen or —CH₃; or R(1), R(2) and R(3) independently of one anotherare —Q4-[(CH₂)_(k)—CHR(17)—(C═O)R(20)]-phenyl,—Q-3—(CH₂)_(k)—CHR(17)—(C═O)R(20)]-phenyl or—Q-2-[(CH₂)_(k)—CHR(17)—(C═O)R(20)]-phenyl, where the phenyl in eachcase is unsubstituted or substituted by 1-2 substituents from the groupF, Cl, —CF₃, methyl, hydroxyl, methoxy and —NR(35)R(36); R(35) and R(36)independently of one another are hydrogen or —CH₃; Q is a bond, oxygen,—S— or —NR(18); R(18) is hydrogen or —(C₁-C₄)-alkyl; R(17) is —OR(21) or—NR(21)R(22); R(21) and R(22) independently of one another are hydrogen,—(C₁-C₈)-alkyl, —(C₁-C₈)-alkanoyl, —(C₁-C₈)-alkoxycarbonyl, benzyl orbenzyloxycarbonyl; or R(21) is trityl; R(20) is —OR(23) or —NR(23)R(24);R(23), R(24) independently of one another are hydrogen, —(C₁-C₈)-alkylor benzyl; k is zero, 1, 2, 3 or 4; or R(1), R(2) and R(3) independentlyof one another are (C₁-C₉)-heteroaryl, which is linked via C or N andwhich is unsubstituted or substituted by 1-3 substituents from the groupF, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; or R(1), R(2) and R(3) are —SR(25), —OR(25), —NR(25)R(26)or —CR(25)R(26)R(27); R(25) is —C_(f)H_(2f)—(C₁-C₉)-heteroaryl, which isunsubstituted or substituted by 1-3 substituents from the group F, Cl,CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; f iszero, 1 or 2; R(26) and R(27) independently of one another are definedas R(25) or are hydrogen or (C₁-C₄)-alkyl, or R(1), R(2) and R(3)independently of one another are (C₁-C₉)-heteroaryl-N-oxide, which islinked via C or N and which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; or R(1), R(2)and R(3) independently of one another are —SR(28), —OR(28), —NR(28)R(29)or —CR(28)R(29)R(30); R(28) is —C_(g)H_(2g)—(C₁-C₉)-heteroaryl-N-oxide,which is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; g is zero, 1 or 2; R(29), R(30)independently of one another are defined as R(28), hydrogen or(C₁-C₄)-alkyl; or R(1), R(2) and R(3) independently of one another arehydrogen, F, Cl, Br, I, —C≡N, T—(CH₂)_(h)—(C_(i)F_(2i+1)), R(31)SO_(I)—,R(32)R(33)N—CO—, R(34)—CO— or R(45)R(46)N—SO₂, where the perfluoroalkylgroup is straight-chain or branched; T is a bond, oxygen, —S— or—NR(47); I is zero, 1 or 2; h is zero, 1 or 2; i is 1, 2, 3, 4, 5 or 6;R(31), R(32), R(34) and R(45) independently of one another are—(C₁-C₈)-alkyl, —(C₃-C₆)-alkenyl, (CH₂)_(n)R(48) or —CF₃; n is zero, 1,2, 3 or 4; R(47) is hydrogen or alkyl with 1, 2 or 3 carbon atoms; R(48)is —(C₃-C₇)-cycloalkyl or phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, —CF₃, methyl, methoxy and —NR(49)R(50); R(49) and R(50) are hydrogenor alkyl having 1, 2, 3 or 4 carbon atoms; or R(32), R(34) and R(45) arehydrogen; R(33) and R(46) independently of one another are hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms; or R(32) and R(33), and R(45)and R(46) together are 5 or 6 methylene groups, of which one CH₂ groupcan be replaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl; or R(1), R(2)and R(3) independently of one another are R(51)—A-G-D-; R(51) is anamino group —NR(52)R(53), an amidino group R(52)R(53)N—C[═N—R(54)]— or aguanidino group R(52)R(53)N—C[═N—R(54)]—NR(55)—; R(52), R(53), R(54) andR(55) independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms; or R(52) and R(53) are a group C_(γ)H_(2γ); γ is 4,5, 6 or 7; where if γ=5, 6 or 7 a carbon atom of the group C_(γ)H_(2γ)can be replaced by a heteroatom group O, SO_(d) or NR(56), or R(53) andR(54) or R(54) and R(55) or R(52) and R(55) are a group C_(y)H_(2y); yis 2, 3, 4 or 5; where if y=3, 4 or 5 a carbon atom of the groupC_(y)H_(2y) can be replaced by a heteroatom group O, SO_(d) or NR(56); dis zero, 1 or 2; R(56) is hydrogen or methyl; or R(51) is a basicheteroaromatic ring system having 1-9 carbon atoms; A is a groupC_(e)H_(2e); e is zero, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 1; where in thegroup C_(e)H_(2e) a carbon atom can be replaced by one of the groupings—O—, —CO—, or —SO_(r)—; r is zero, 1 or 2; G is a phenylene radical

R(58) and R(59) independently of one another are hydrogen, methyl,methoxy, F, Cl, Br, I, CF₃ or —So_(s)—R(60); s is zero, 1 or 2; R(60) ismethyl or NR(61)R(62);  R(61) and R(62)  independently of one anotherare hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; D is—C_(v)H_(2v)—E_(w)—; v is zero, 1, 2, 3 or 4; E is —O—, —CO—,—CH[OR(63)]—, —SO_(aa)— or —NR(63)—; w is zero or 1; aa is zero, 1 or 2R(63) is hydrogen or methyl, or R(1), R(2) and R(3) independently of oneanother are —CF₂R(64), —CF[R(65)][R(66)], —CF[(CF₂)_(q)—CF₃)][R(65)] or—C[(CF₂)_(p)—CF₃]═CR(65)R(66); R(64) is alkyl having 1, 2, 3 or 4 carbonatoms or cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; R(65) and R(66)independently of one another are hydrogen or alkyl having 1, 2, 3 or 4carbon atoms; q is zero, 1 or 2; p is zero, 1 or 2; or R(1), R(2) andR(3) independently of one another are —OR(67) or —NR(67)R(68); R(67) andR(68) independently of one another are hydrogen or alkyl having 1, 2, 3,4, 5 or 6 carbon atoms; or R(67) and R(68) together are 4, 5, 6 or 7methylene groups, of which one CH₂ group can be replaced by oxygen, —S—,SO₂, —NH—, —NCH₃ or —N-benzyl; R(4) and R(5) independently of oneanother are hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, F, Cl,—OR(69), —NR(70)R(71) or —C_(z)F_(2z+1); R(69), R(70) and R(71)independently of one another are hydrogen or alkyl having 1, 2 or 3carbon atoms; z is 1, 2, 3 or 4; R(6) and R(7) independently of oneanother are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; X isoxygen or NR(72); R(72) is hydrogen or alkyl having 1, 2, 3 or 4 carbonatoms; or pharmaceutically tolerable salt thereof; al) analkenylcarboxylic acid guanidide of the formula

in which: R(6) is hydrogen, (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl or phenyl,where the phenyl group is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(9)R(10); R(9) and R(10) are hydrogen, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; R(7) independently is defined as R(6); R(1),R(2), R(3), R(4) and R(5) independently of one another are hydrogen orF; where, however, at least one of the radicals R(1), R(2), R(3), R(4)and R(5) must be fluorine; or pharmaceutically tolerable salt thereof;am) a benzoylguanidine of the formula

in which: R(1) is R(4)—SO_(m) or R(5)R(6)N—SO₂—; m is 1 or 2; R(4) andR(5) independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms, alkenyl having 3, 4, 5 or 6 carbon atoms, CF₃ or—C_(n)H_(2n)—R(7); n is zero, 1, 2, 3 or 4; R(6) is H or alkyl having 1,2, 3 or 4 carbon atoms; R(7) is cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms or phenyl, which is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(8)R(9); R(8) and R(9)  are H or alkyl having 1,2, 3 or 4 carbon atoms; or R(5) is also hydrogen; or R(5) and R(6)together are 4 or 5 methylene groups, of which a CH₂ group can bereplaced by oxygen, S, NH, N—CH₃ or N-benzyl; or R(1) is—O_(p)—(CH₂)_(q)—(CF₂)_(r)—CF₃; p is zero or 1; q is zero, 1 or 2; r iszero, 1, 2 or 3; or R(1) is —SR(10), —OR(10) or —CR(10)R(11)R(12);R(10), R(11) and R(12) independently of one another are hydrogen, alkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,—C_(s)H_(2s)—(C₃-C₈)-cycloalkyl or an aromatic system selected from thegroup consisting of pyridyl, pyrrolyl, quinolyl, isoquinolyl, imidazolyland phenyl; s is zero, 1 or 2; where the aromatic systems pyridyl,pyrrolyl, quinolyl, isoquinolyl, imidazolyl and phenyl are unsubstitutedor substituted by 1-3 substituents selected from the group consisting ofF, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; R(2) is —(CH₂)_(u)—(CF₂)_(t)—CF₃; t is zero, 1, 2 or 3; uis zero or 1; R(3) is hydrogen or independently is defined as R(1); orpharmaceutically tolerable salt thereof; an) a substituted cinnamic acidguanidide of the formula

in which: at least one of the substituents R(1), R(2), R(3), R(4) andR(5) is —X_(a)—Y_(b)—L_(n)—U; X is CR(16)R(17), O, S or NR(18); R(16),R(17) and R(18) independently of one another are H, alkyl having 1, 2, 3or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; ais zero or 1; Y is alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, alkylene-T having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms in thealkylene group, T, T-alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms in the alkylene group; T is NR(20), O, S or phenylene, where thephenylene is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(21)R(22); R(20), R(21) and R(22)  independently of one another are H,alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3or 4 carbon atoms; b is zero or 1; L is O, S, NR(23) or C_(k)H_(2k); kis 1, 2, 3, 4, 5, 6, 7 or 8; n is zero or 1; U is NR(24)R(25) or anN-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms; R(24) and R(25) independently of one another are hydrogen, alkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or perfluoroalkyl having 1,2, 3, 4, 5, 6, 7 or 8 carbon atoms; or R(24) and R(25) together are 4 or5 methylene groups, of which one CH₂ group can be replaced by oxygen, S,NH, N—CH₃ or N-benzyl;  where the N-containing heterocycles are N- orC-bridged and are not substituted or are substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(27)R(28); R(23), R(27) and R(28) independently of one another are H,alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3or 4 carbon atoms; and the other substituents R(1), R(2), R(3), R(4) andR(5) in each case independently of one another are H, F, Cl, Br, I, CN,—O_(n)—C_(m)H_(2m+1), —O_(p)—(CH₂)_(s)—C_(q)F_(2q+1) or—C_(r)H_(2r)R(10); n is zero or 1; m is zero, 1, 2, 3, 4, 5, 6, 7 or 8;p is zero or 1; q is 1, 2, 3, 4, 5, 6, 7 or 8; s is zero, 1, 2, 3 or 4;r is zero, 1, 2, 3 or 4; R(10) is cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms, or phenyl, where the phenyl is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(11)R(12); R(11) and R(12)  independentlyof one another are H, alkyl having 1, 2, 3 or 4 carbon atoms orperfluoroalkyl having 1, 2, 3 or 4 carbon atoms; R(6) and R(7)independently of one another are hydrogen, F, Cl, Br, I, CN, alkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, perfluoroalkyl having 1,2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms, or phenyl, which is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(14)R(15); R(14) and R(15) independently of oneanother are H, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms; or pharmaceutically tolerable saltthereof; ao) a benzoylguanidine of the formula

in which: at least one of the substituents R(1), R(2) and R(3) isR(6)—C(OH)₂—; R(6) is perfluoroalkyl having 1, 2 or 3 carbon atoms,which is straight-chain or branched; and the other substituents R(1),R(2) and R(3) independently of one another are hydrogen, OH, F, Cl, Br,I, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, cycloalkyl having 3, 4,5 or 6 carbon atoms, alkoxy having 1, 2, 3 or 4 carbon atoms, orphenoxy, which is unsubstituted or is substituted by 1-3 substituentsselected from the group consisting of F, Cl, methyl and methoxy; or theother substituents R(1), R(2) and R(3) independently of one another arealkyl-SO_(x), —CR(7)═CR(8)R(9) or —C≡CR(9); x is zero, 1 or 2; R(7) ishydrogen or methyl; R(8) and R(9) independently of one another arehydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, cycloalkyl having 3,4, 5, 6, 7 or 8 carbon atoms, or phenyl, which is unsubstituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl and methoxy; or the other substituents R(1), R(2) andR(3) independently of one another are phenyl, C₆H₅—(C₁-C₄)-alkyl,naphthyl, biphenylyl, quinolinyl, isoquinolinyl or imidazolyl, wherequinolinyl, isoquinolinyl or imidazolyl are bonded via C or N and wherephenyl, C₆H₅—(C₁-C₄)-alkyl, naphthyl, biphenylyl, quinolinyl,isoquinolinyl and imidazolyl are unsubstituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; or the othersubstituents R(1), R(2) and R(3) independently of one another areSR(10), —OR(10), —CR(10)R(11)R(12); R(10) is—C_(f)H_(2f)—(C₃-C₈)-cycloalkyl, quinolinyl, isoquinolinyl, pyridinyl,imidazolyl or phenyl, where the aromatic systems quinolinyl,isoquinolinyl, pyridinyl, imidazolyl and phenyl are unsubstituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; fis zero, 1 or 2; R(11) and R(12) independently of one another aredefined as R(10), hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;R(4) and R(5) independently of one another are hydrogen, alkyl having 1,2 or 3 carbon atoms, F, Cl, Br, I, CN, OR(13), NR(14)R(15) or—(CH₂)_(n)—(CF₂)_(o)—CF₃; R(13), R(14) and R(15) independently of oneanother are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; n iszero or 1; o is zero, 1 or 2; or pharmacologically acceptable saltthereof; ap) a sulfonimidamide of the formula

in which: at least one of the three substituents R(1), R(2) and R(3) isa benzoylguanidine,

which is unsubstituted or substituted in the phenyl moiety by 1-4radicals selected from the group consisting of alkyl having 1, 2, 3, 4,5, 6, 7 or 8 carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbonatoms, —(CH₂)_(m)—R(14), F, Cl, Br, I, —C≡N, CF₃, R(22)SO₂—,R(23)R(24)N—CO—, R(25)—CO—, R(26)R(27)N—SO₂, —OR(35), —SR(35) or—NR(35)R(36); m is zero, 1 or 2; R(14) is —(C₃-C₈)-cycloalkyl or phenyl,which is not substituted or is substituted by 1-3 substituents selectedfrom the group consisting of F and Cl, —CF₃, methyl, methoxy and—NR(15)R(16); R(15) and R(16)  independently of one another are hydrogenor —CH₃; R(22), R(23), R(25) and R(26) independently of one another arealkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, alkenyl having 2, 3,4, 5, 6, 7 or 8 carbon atoms, (CH₂)_(n)R(29) or —CF₃; n is zero, 1, 2, 3or 4; R(29) is —(C₃-C₇)-cycloalkyl or phenyl, which is not substitutedor is substituted by 1-3 substituents selected from the group consistingof F, Cl, —CF₃, methyl, methoxy and —NR(30)R(31); R(30) and R(31)  arehydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; or R(23), R(25) andR(26) are hydrogen; R(24) and R(27) independently of one another arehydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; or R(23) and R(24),and also R(26) and R(27) together are 5 or 6 methylene groups, of whichone CH₂ group can be replaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;R(35) and R(36) independently of one another are hydrogen or alkylhaving 1, 2, 3, 4, 5 or 6 carbon atoms; or R(35) and R(36) together are4-7 methylene groups, of which one CH₂ group can be replaced by oxygen,—S—, —NH—, —NCH₃ or —N-benzyl; or R(35) is phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, —CF₃, methyl, methoxy, SO₂R(5), SO₂NR(6)R(7)and —NR(32)R(33); R(5) is alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms;R(6) and R(7) independently of one another are hydrogen or alkyl having1, 2, 3 or 4 carbon atoms; R(32) and R(33) independently of one anotherare hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; or R(35) isC₁-C₉-heteroaryl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; and the othersubstituents R(1), R(2) and R(3) in each case independently of oneanother are alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,(CH₂)_(p)R(10); p is zero, 1, 2, 3 or 4; R(10) is phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, —CF₃, methyl, methoxy, —SO₂NR(17)R(8) and—SO₂R(9); R(17) and R(8) independently of one another are hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms; R(9) is alkyl having 1, 2, 3 or4 carbon atoms; or the other radical R(1) or R(3) in each case ishydrogen, R(4) is hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; orpharmaceutically tolerable salt thereof; aq) a benzoylguanidine of theformula

in which: R(1) is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms orNR(7)R(8); R(7) and R(8) independently of one another are hydrogen oralkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; R(2) is hydrogen,alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or —SO₂R(9); R(9)independently is defined as R(1); R(3) is hydrogen, —SR(25), —OR(25),—NR(25)R(26) or —CR(25)R(26)R(27); R(25) is hydrogen, alkyl having 1, 2,3, 4, 5, 6, 7 or 8 carbon atoms, or phenyl, which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;or R(25) is —(C₁-C₉)-heteroaryl, which is unsubstituted or substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; R(26) andR(27) independently of one another are defined as R(25) or are hydrogenor alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; R(4) is hydrogen,F, Cl, Br, I, OH, —C≡N, CF₃, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms or—(CH₂)_(m)R(14); m is zero, 1 or 2; R(14) is —(C₃-C₈)-cycloalkyl orphenyl, which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16); R(15) and R(16) independently of one another arehydrogen or —CH₃; R(5) and R(6) independently of one another arehydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, F, Cl, —OR(32),—NR(33)R(34) or CF₃; R(32), R(33) and R(34) independently of one anotherare hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; orpharmaceutically tolerable salt thereof; ar) a benzenedicarboxylic aciddiguanidide of the formula

in which: one of the radicals R(1), R(2), R(3) and R(4) is—CO—N═C(NH₂)₂; and of the other radicals R(1), R(2), R(3) and R(4) ineach case: R(1) is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, F,Cl, Br, I, —OR(32), —NR(33)R(34) or CF₃; R(32), R(33) and R(34)independently of one another are hydrogen or alkyl having 1, 2, 3 or 4carbon atoms; R(2) and R(4) independently of one another are hydrogen,F, Cl, Br, I, OH, —CN, CF₃, —CO—N═C(NH₂)₂, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbonatoms or —(CH₂)_(m)R(14); m is zero, 1 or 2; R(14) is—(C₃-C₈)-cycloalkyl or phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of Fand Cl, —CF₃, methyl, methoxy and —NR(15)R(16); R(15) and R(16) arehydrogen or —CH₃; or R(2) and R(4) independently of one another arepyrrol-1-yl, pyrrol-2-yl or pyrrol-3-yl, which is not substituted or issubstituted by 1-4 substituents selected from the group consisting of F,Cl, Br, I, —CN, (C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl,carboxyl, —CF₃, methyl and methoxy; or R(2) and R(4) independently ofone another are R(22)—SO₂—, R(23)R(24)N—CO—, R(28)—CO— orR(29)R(30)N—SO₂; R(22) and R(28) independently of one another are methylor —CF₃; R(23), R(24), R(29) and R(30) independently of one another arehydrogen or methyl; or R(2) and R(4) independently of one another are—OR(35) or —NR(35)R(36); R(35) and R(36) independently of one anotherare hydrogen or alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms; or R(35)and R(36) together are 4-7 methylene groups, of which one CH₂ group canbe replaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl; R(3) is hydrogen,—SR(25), —OR(25), —NR(25)R(26) or —CR(25)R(26)R(27); R(25) is hydrogen,alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or phenyl, which isunsubstituted or substituted by 1-3 substituents selected from the groupconsisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; or R(25) is —(C₁-C₉)-heteroaryl, which is unsubstitutedor substituted by 1-3 substituents selected from the group consisting ofF, Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino anddimethylamino; R(26) and R(27) independently of one another are definedas R(25) or are hydrogen or alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms; R(5) is alkyl having 1, 2, 3 or 4 carbon atoms, F, Cl, Br, I,X—(CH₂)_(y)—CF₃ or phenyl, which is not substituted or is substituted by1-3 substituents selected from the group consisting of F and Cl, —CF₃,methyl, methoxy and —NR(6)R(7); R(6) and R(7) independently of oneanother are hydrogen or —CH₃; X is a bond or oxygen; y is zero, 1 or 2;or pharmaceutically tolerable salt thereof; as) a benzenedicarboxylicacid diguanidide of the formula

in which: one of the radicals R(1), R(2), R(3) and R(5) is—CO—N═C(NH₂)₂; and of the other radicals R(1), R(2), R(3) and R(5) ineach case: R(1) and R(5) independently of one another are hydrogen,alkyl having 1, 2, 3 or 4 carbon atoms, F, Cl, —OR(32), —NR(33)R(34) orCF₃; R(32), R(33) and R(34) independently of one another are hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms; R(2) is hydrogen, F, Cl, Br, I,OH, —CN, CF₃, —CO—N═C(NH₂)₂, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms or—(CH₂)_(m)R(14); m is zero, 1 or 2; R(14) is —(C₃-C₈)-cycloalkyl orphenyl, which is not substituted or is substituted by 1-3 substituentsselected from the group consisting of F and Cl, —CF₃, methyl, methoxyand —NR(15)R(16); R(15) and R(16) independently of one another arehydrogen or —CH₃; or R(2) is R(22)—SO₂—, R(23)R(24)N—CO—, R(28)—CO— orR(29)R(30)N—SO₂; R(22) and R(28) independently of one another are methylor —CF₃; R(23), R(24), R(29) and R(30) independently of one another arehydrogen or methyl; or R(2) is —OR(35) or —NR(35)R(36); R(35) and R(36)independently of one another are hydrogen or alkyl having 1, 2, 3, 4, 5or 6 carbon atoms; or R(35) and R(36) together are 4-7 methylene groups,of which one CH₂ group can be replaced by oxygen, —S—, —NH—, —NCH₃ or—N-benzyl; R(3) is hydrogen, —SR(25), —OR(25), —NR(25)R(26),—CR(25)R(26)R(27); R(25) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms, or phenyl, which is unsubstituted or substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; or R(25) is—(C₁-C₉)-heteroaryl, which is unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; R(26) and R(27)independently of one another are defined as R(25) or are hydrogen oralkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; R(4) is CF₃, alkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, alkenyl having 2, 3, 4, 5,6, 7 or 8 carbon atoms, —(C₃-C₈)-cycloalkyl or —(CH₂)_(m)R(14); m is 1or 2; R(14) is —(C₃-C₈)-cycloalkyl or phenyl, which is not substitutedor is substituted by 1-3 substituents selected from the group consistingof F and Cl, —CF₃, methyl, methoxy and —NR(15)R(16); R(15) and R(16)independently of one another are hydrogen or —CH₃; or R(4) is phenyl,which is substituted by 2, 3, 4 or five substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and —NR(15)R(16); R(15)and R(16) independently of one another are hydrogen or CH₃; orpharmaceutically tolerable salt thereof; at) a diaryldicarboxylic aciddiguanidide of the formula

in which: one of the radicals R(1), R(2), R(3), R(4) and R(5) is—CO—N═C(NH₂)₂; the other radicals R(1) and R(5) in each caseindependently of one another are hydrogen, alkyl having 1, 2, 3 or 4carbon atoms, F, Cl, —OR(32), —NR(33)R(34) or CF₃; R(32), R(33) andR(34) independently of one another are hydrogen or alkyl having 1, 2, 3or 4 carbon atoms; the other radicals R(2) and R(4) in each caseindependently of one another are hydrogen, F, Cl, Br, I, OH, —CN, CF₃,—CO—N═C(NH₂)₂, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkenyl having 2, 3, 4, 5, 6, 7 or 8 carbon atoms or —(CH₂)_(m)R(14); mis zero, 1 or 2; R(14) is —(C₃-C₈)-cycloalkyl or phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F and Cl, —CF₃, methyl, methoxy and —NR(15)R(16);R(15) and R(16) are hydrogen or —CH₃; or the other radicals R(2) andR(4) in each case independently of one another are pyrrol-1-yl,pyrrol-2-yl or pyrrol-3-yl, which is not substituted or is substitutedby 1-4 substituents selected from the group consisting of F, Cl, Br, I,—CN, (C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃,methyl and methoxy; or the other radicals R(2) and R(4) in each case areR(22)—SO₂—, R(23)R(24)N—CO—, R(28)—CO— or R(29)R(30)N—SO₂; R(22) andR(28) independently of one another are methyl or —CF₃; R(23), R(24),R(29) and R(30) independently of one another are hydrogen or methyl; orthe other radicals R(2) and R(4) in each case independently of oneanother are —OR(35) or —NR(35)R(36); R(35) and R(36) independently ofone another are hydrogen or alkyl having 1, 2, 3, 4, 5 or 6 carbonatoms; or R(35) and R(36) together are 4-7 methylene groups, of whichone CH₂ group can be replaced by oxygen, —S—, —NH—, —NCH₃ or —N-benzyl;the other radical R(3) in each case is hydrogen, —SR(25), —OR(25),—NR(25)R(26), —CR(25)R(26)R(27); R(25) is hydrogen, alkyl having 1, 2,3, 4, 5, 6, 7 or 8 carbon atoms, or phenyl, which is unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino;or R(25) is —(C₁-C₉)-heteroaryl, which is unsubstituted or substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; R(26) andR(27) independently of one another are defined as R(25) or are hydrogenor alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; one of theradicals R(6), R(7), R(8), R(9) and R(10) is —CO—N═C(NH₂)₂; the otherradicals R(6) and R(10) in each case independently of one another arehydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, F, Cl, —OR(132),—NR(133)R(134) or CF₃; R(132), R(133) and R(134) independently of oneanother are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; theother radicals R(7) and R(9) in each case independently of one anotherare hydrogen, F, Cl, Br, I, OH, —CN, CF₃, —CO—N═C(NH₂)₂, alkyl having 1,2, 3, 4, 5, 6, 7 or 8 carbon atoms, alkenyl having 2, 3, 4, 5, 6, 7 or 8carbon atoms or —(CH₂)_(mm)R(114); mm is zero, 1 or 2; R(114) is—(C₃-C₈)-cycloalkyl or phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of Fand Cl, —CF₃, methyl, methoxy and —NR(115)R(116); R(115) and R(116)  arehydrogen or —CH₃; or the other radicals R(7) and R(9) in each caseindependently of one another are pyrrol-1-yl, pyrrol-2-yl orpyrrol-3-yl, which is not substituted or is substituted by 1-4substituents selected from the group consisting of F, Cl, Br, I, —CN,(C₂-C₈)-alkanoyl, (C₂-C₈)-alkoxycarbonyl, formyl, carboxyl, —CF₃, methyland methoxy; or the other radicals R(7) and R(9) in each case areR(122)—SO₂—, R(123)R(124)N—CO—, R(128)—CO— or R(129)R(130)N—SO₂; R(122)and R(128) independently of one another are methyl or —CF₃; R(123),R(124), R(129) and R(130) independently of one another are hydrogen ormethyl; or the other radicals R(7) and R(9) in each case independentlyof one another are —OR(135) or —NR(135)R(136); R(135) and R(136)independently of one another are hydrogen or alkyl having 1, 2, 3, 4, 5or 6 carbon atoms; or R(135) and R(136) together are 4-7 methylenegroups, of which one CH₂ group can be replaced by oxygen, —S—, —NH—,—NCH₃ or —N-benzyl; the other radical R(8) in each case is hydrogen,—SR(125), —OR(125), —NR(125)R(126) or —CR(125)R(126)R(127); R(125) ishydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or phenyl,which is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; or R(125) is —(C₁-C₉)-heteroaryl, whichis unsubstituted or substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; R(126) and R(127) independently of oneanother are defined as R(125) or are hydrogen or alkyl having 1, 2, 3,4, 5, 6, 7 or 8 carbon atoms; A is absent or is —NR(11)—CO—,—NR(12)—CO—NR(13)—, —NR(17)—CO—NR(18)—SO₂—, —NR(19)—SO₂—,—SO₂—NR(19)—SO₂—, —SO₂—NR(19)—CO—, —O—CO—NR(19)—SO₂— or —CR(20)═CR(21)—;R(11), R(12), R(13), R(17), R(18), R(19), R(20) and R(21) independentlyof one another are hydrogen or alkyl having 1, 2, 3, 4, 5, 6, 7 or 8carbon atoms or pharmaceutically tolerable salt thereof; au) asubstituted thiophenylalkenylcarboxylic acid guanidide of the formula

in which: at least one of the substituents R(1), R(2) and R(3) is—O_(p)—(CH₂)_(s)—C_(q)F_(2q+1), R(40)CO— or R(31)SO_(k)—; p is zero or1; s is zero, 1, 2, 3 or 4; q is 1, 2, 3, 4, 5, 6, 7 or 8; k is zero, 1or 2; R(40) is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkylhaving 3, 4, 5, 6, 7 or 8 carbon atoms, or phenyl, which is notsubstituted or is substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl and methoxy; R(31) is alkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, perfluoroalkyl having 1,2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms, or phenyl, which is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl and methoxy; or R(31) is NR(41)R(42); R(41) and R(42)independently of one another are hydrogen, alkyl having 1, 2, 3 or 4carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms, orR(41) and R(42) together are 4 or 5 methylene groups, of which one CH₂group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl; and the othersubstituents R(1), R(2) and R(3) in each case independently of oneanother are H, F, Cl, Br, I, CN, —O_(na)—C_(ma)H_(2ma+1) or—O_(ga)C_(ra)H_(2ra)R(10); na is zero or 1; ma is zero, 1, 2, 3, 4, 5,6, 7 or 8; ga is zero or 1; ra is zero, 1, 2, 3 or 4; R(10) iscycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms or phenyl, where thephenyl is not substituted or is substituted by 1-3 substituents selectedfrom the group consisting of F, Cl, CF₃, methyl and methoxy; R(4) andR(5) independently of one another are hydrogen, F, Cl, Br, I, CN, alkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, perfluoroalkyl having 1,2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms or phenyl, which is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(14)R(15); R(14) and R(15) independently of oneanother are H, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms; or pharmaceutically tolerable saltthereof; av) an ortho-substituted benzoylguanidine of the formula

in which: R(2) and R(3) independently of one another are hydrogen, Cl,Br, I, (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl or —OR(5); R(5) is(C₁-C₈)-alkyl or —C_(d)H_(2d)—(C₃-C₈)-cycloalkyl; d is zero, 1 or 2;where one of the two substituents R(2) and R(3) is always hydrogen butboth substituents R(2) and R(3) are not simultaneously hydrogen, orpharmaceutically tolerable salt thereof; aw) a benzoylguanidine of theformula

in which: R(1) is H, F, Cl, Br, I, CN, NO₂, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms, alkoxy having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkoxyhaving 3, 4, 5, 6, 7 or 8 carbon atoms or X_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃;X is oxygen, S, NR(5), a is zero or 1; b is zero, 1 or 2; c is zero, 1,2 or 3; R(5) is H, alkyl having 1, 2, 3 or 4 carbon atoms or—C_(d)H_(2d)R(6); d is zero, 1, 2, 3 or 4; R(6) is cycloalkyl having 3,4, 5, 6, 7 or 8 carbon atoms, phenyl, biphenylyl or naphthyl, where thearomatics phenyl, biphenylyl or naphthyl are not substituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(7)R(8); R(7) and R(8)  independently areH or alkyl having 1, 2, 3 or 4 carbon atoms; or R(1) is —SR(10), —OR(10)or —CR(10)R(11)R(12); R(10) is —C_(f)H_(2f)-cycloalkyl having 3, 4, 5,6, 7 or 8 carbon atoms in the cycloalkyl ring, or phenyl, where phenylis unsubstituted or substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; f is zero, 1 or 2; R(11) and R(12)independently of one another are defined as R(10) or are hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms; or R(1) is phenyl, naphthyl,biphenylyl or heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms, with the latter being linked via a carbon atom or a nitrogen atomof the ring, which are in each case unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino, or R(1) is—SR(13), —OR(13), —NHR(13), —NR(13)R(14), —CHR(13)R(15),—C[R(15)R(16)OH], —C≡CR(18), —C[R(19)]═CHR(18) or —C[R(20) R(21)]_(k)—(CO)—[CR(22)R(23)]_(l)—R(24), k is zero, 1, 2, 3 or 4; l iszero, 1, 2, 3 or 4; R(13) and R(14) identically or differently are—(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(j—R()17) or—(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(24); R(17) is hydrogen or methyl, g, h andi identically or differently are zero, 1, 2, 3 or 4; j is 1, 2, 3 or 4;R(15) and R(16) identically or differently are hydrogen, alkyl having 1,2, 3, 4, 5 or 6 carbon atoms or, together with the carbon atom carryingthem, are cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms; R(18) isphenyl, which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(25)R(26); R(25) and R(26)  are H or alkyl having 1, 2, 3 or 4 carbonatoms; or R(18) is heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms, which is unsubstituted or substituted as phenyl; or R(18) isalkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, which is unsubstituted orsubstituted by 1-3 OH; or R(18) is cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms; R(19), R(20), R(21), R(22) and R(23) identically ordifferently are hydrogen or methyl; R(24) is H, alkyl having 1, 2, 3, 4,5 or 6 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atomsor C_(m)H_(2m)—R(18); m is 1, 2, 3 or 4; R(2) and R(3) are defined asR(1); R(4) is alkyl having 1, 2, 3 or 4 carbon atoms; orpharmaceutically tolerable salt thereof; ax) an ortho-substitutedbenzoylguanidine of the formula

in which: R(1) is H, F, Cl, Br, I, CN, NO₂, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms, alkoxy having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkoxyhaving 3, 4, 5, 6, 7 or 8 carbon atoms or X_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃;X is oxygen, S, NR(5), a is zero or 1; b is zero, 1 or 2; c is zero, 1,2 or 3; R(5) is H, alkyl having 1, 2, 3 or 4 carbon atoms or—C_(d)H_(2d)R(6); d is zero, 1, 2, 3 or 4; R(6) is cycloalkyl having 3,4, 5, 6, 7 or 8 carbon atoms, phenyl, biphenylyl or naphthyl,  where thearomatics phenyl, biphenylyl or naphthyl are not substituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(7)R(8);  R(7) and R(8)  independentlyare H or alkyl having 1, 2, 3 or 4 carbon atoms; or R(1) is —SR(10),—OR(10) or —CR(10)R(11)R(12); R(10) is —C_(f)H_(2f)-cycloalkyl having 3,4, 5, 6, 7 or 8 carbon atoms in the cycloalkyl ring, or phenyl, wherephenyl is unsubstituted or substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, CH₃, methoxy, hydroxyl, amino,methylamino and dimethylamino; f is zero, 1 or 2; R(11) and R(12)independently of one another are defined as R(10), or are hydrogen oralkyl having 1, 2, 3 or 4 carbon atoms; or R(1) is phenyl, naphthyl,biphenylyl or heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms, with the latter being linked via a carbon atom or a nitrogen atomof the ring, which are in each case unsubstituted or substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino, or R(1) is—SR(13), —OR(13), —NHR(13), —NR(13)R(14), —CHR(13)R(15),—C[R(15)R(16)OH], —C≡CR(18), —C[R(19)]═CHR(18) or—C[R(20)R(21)]_(k)—(CO)—[CR(22)R(23)]_(l)—R(24), k is zero, 1, 2, 3 or4; l is zero, 1, 2, 3 or 4; R(13) and R(14) identically or differentlyare —(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(j)—R(17) or—(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(24); R(17) is hydrogen or methyl, g, h andi identically or differently are zero, 1, 2, 3 or 4; j is 1, 2, 3 or 4;R(15) and R(16) identically or differently are hydrogen, alkyl having 1,2, 3, 4, 5 or 6 carbon atoms or, together with the carbon atom carryingthem, are cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms; R(18) isphenyl, which is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(25)R(26); R(25) and R(26)  are H or alkyl having 1, 2, 3 or 4 carbonatoms; or R(18) is heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbonatoms, which is unsubstituted or substituted as phenyl; or R(18) isalkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, which is unsubstituted orsubstituted by 1-3 OH; or R(18) is cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms; R(19), R(20), R(21), R(22) and R(23) identically ordifferently are hydrogen or methyl; R(24) is H, alkyl having 1, 2, 3, 4,5 or 6 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atomsor —C_(m)H_(2m)—R(18); m is 1, 2, 3 or 4; one of the two substituentsR(2) and R(3) is hydroxyl; and the other of the substituents R(2) andR(3) in each case is defined as R(1); R(4) is alkyl having 1, 2, 3 or 4carbon atoms; alkoxy having 1, 2, 3 or 4 carbon atoms, F, Cl, Br, I or—(CH₂)_(n)—(CF₂)_(o)—CF₃; n is zero or 1; o is zero or 1; orpharmaceutically tolerable salt thereof; ay) a bis-ortho-substitutedbenzoylguanidine of the formula

in which: R(1), R(2) and R(3) independently of one another areR(10)—SO_(a)— or R(14)R(15)N—SO₂—; a is zero, 1 or 2, R(10), R(14) andR(15) independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7or 8 carbon atoms, perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, alkenyl having 3, 4, 5 or 6 carbon atoms or —C_(ab)H_(2ab)—R(16);ab is zero, 1, 2, 3 or 4; R(16) is cycloalkyl having 3, 4, 5, 6 or 7carbon atoms, or phenyl, which is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(17)R(18); R(17) and R(18)  independently of oneanother are hydrogen, CF₃ or alkyl having 1, 2, 3 or 4 carbon atoms; orR(14) and R(15) together are 4 or 5 methylene groups, of which one CH₂group can be replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl; or R(14)and R(15) are hydrogen; or R(1), R(2) and R(3) independently of oneanother are SR(21), —OR(22), —NR(23)R(24) or —CR(25)R(26)R(27); R(21),R(22), R(23) and R(25) independently of one another are—C_(b)H_(2b)—(C₁-C₉)-heteroaryl, which is unsubstituted or substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,CH₃, methoxy, hydroxyl, amino, methylamino and dimethylamino; b is zero,1 or 2; R(24), R(26) and R(27) independently of one another arehydrogen, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms; or R(1), R(2) and R(3) independentlyof one another are hydrogen, F, Cl, Br, I, CN,(X_(a))_(dg)—C_(da)H_(2da+1), —(Xb)_(dh)—(CH₂)_(db)—C_(de)F_(2de+1),alkenyl having 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(df)H_(2df)R(30);(X_(a)) is oxygen, sulfur or NR(33); R(33) is hydrogen, alkyl having 1,2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms; dg is zero or 1; (Xb) is oxygen, sulfur or NR(34); R(34) ishydrogen, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms; dh is zero or 1; da is zero, 1, 2, 3,4, 5, 6, 7 or 8; db is zero, 1, 2, 3 or 4; de is zero, 1, 2, 3, 4, 5, 6or 7; df is zero, 1, 2, 3 or 4; R(30) is cycloalkyl having 3, 4, 5, 6, 7or 8 carbon atoms, phenyl, biphenylyl or naphthyl, where the aromaticsphenyl, biphenylyl and naphthyl are not substituted or are substitutedby 1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(31)R(32); R(31) and R(32) are hydrogen, alkylhaving 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4carbon atoms; or R(1), R(2) and R(3) independently of one another areNR(40)R(41) or —(Xe)—(CH₂)_(eb)R(45); R(40) and R(41) independently ofone another are hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or(CH₂)_(e)—R(42); e is zero, 1, 2, 3 or 4; R(42) is cycloalkyl having 3,4, 5, 6 or 7 carbon atoms or phenyl, which is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(43)R(44); R(43) and R(44)  independentlyof one another are hydrogen, CF₃ or alkyl having 1, 2, 3 or 4 carbonatoms; or R(40) and R(41) together are 4 or 5 methylene groups, of whichone CH₂ group can be replaced by oxygen, sulfur, NH, N—CH₃ or N-benzyl;(Xe) is oxygen, sulfur or NR(47); R(47) is hydrogen, alkyl having 1, 2,3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;eb is zero, 1, 2, 3 or 4; R(45) is cycloalkyl having 3, 4, 5, 6 or 7carbon atoms, or phenyl, which is not substituted or is substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy, NR(50)R(51) and —(Xfa)—(CH₂)_(d)—(Xfb)R(46); Xfa isCH₂, oxygen, sulfur or NR(48); Xfb is oxygen, sulfur or NR(49); R(48),R(49), R(50) and R(51)  independently of one another are hydrogen, alkylhaving 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4carbon atoms; ed is 1, 2, 3 or 4; R(46) is hydrogen, alkyl having 1, 2,3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;or R(1), R(2) and R(3) independently of one another are —CHR(52)R(53);R(52) is —(CH₂)_(g)—(CHOH)_(h)—(CH)_(i)—(CHOH)_(k)—R(54) or—(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(54); R(54) is hydrogen or methyl; g, h, iidentically or differently are zero, 1, 2, 3 or 4; k is 1, 2, 3 or 4;R(53) is hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; or R(1),R(2) and R(3) independently of one another are —C(OH)R(55)R(56); R(55)and R(56) identically or differently are hydrogen or alkyl having 1, 2,3 or 4 carbon atoms; or R(55) and R(56) together are cycloalkyl having3, 4, 5 or 6 carbon atoms; or R(55) is —CH₂OH; and R(4) and R(5)independently of one another are alkyl having 1, 2, 3 or 4 carbon atoms,alkoxy having 1, 2, 3 or 4 carbon atoms, OH, F, Cl, Br, I, CN or—O_(n)—(CH₂)_(o)—(CF₂)_(p)—CF₃; n is zero or 1; o is zero, 1 or 2; p iszero, 1 or 2; or pharmaceutically tolerable salt thereof; az) asubstituted 1-naphthoylguanidine of the formula

in which: R2, R3, R4, R5, R6, R7 and RB independently of one another areH, F, Cl, Br, I, CN, NO₂, CF₃, C₂F₅ or X_(a)Y_(b)Z; X is O, S, NR(10),CR(11)R(12), C═O, C(═O)NR(10), C(═O)O, SO, SO₂, SO₂NR(10), OC═O,NR(10)C═O or NR(10)SO₂, where the linkage with the naphthalene ring ineach case takes place via the left atom; R(10), R(11) and R(12)independently of one another are H, alkyl having 1, 2, 3, 4, 5 or 6carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms orcycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; a is zero or 1; Y isalkylene having 1, 2, 3, 4, 5, 6, 7 or 8 CH₂ groups, where one of theseCH₂ groups can be replaced by O, S, NR(13) or o-, p- or m-phenylene;R(13) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3, 4, 5 or 6carbon atoms; b is zero or 1; Z is H, alkyl having 1, 2, 3, 4, 5, 6 or 7carbon atoms, cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms,C(═O)R(15), SO₂R(15), NR(16)R(17) or phenyl, which is not substituted oris substituted by 1-3 substituents selected from the group consisting ofF, Cl, Br, CF₃, methyl, methoxy and NR(21)R(22); R(21) and R(22)independently of one another are H or alkyl having 1, 2, 3 or 4 carbonatoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; R(15) isN═C(NH₂)₂, NR(18)R(19), N(CH₂)_(c)NR(18)R(19) or OR(20); c is 2 or 3;R(18) and R(19)  independently of one another are H, alkyl having 1, 2,3, 4, 5, 6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4carbon atoms; or R(18) and R(19) together are 4 or 5 methylene groups, of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chlorophenyl); R(20) is H, alkyl having 1, 2, 3, 4, 5or 6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms orcycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; R(16) and R(17)independently of one another are H, alkyl having 1, 2, 3, 4, 5, 6, 7 or8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; orR(16) and R(17) together are 4 or 5 methylene groups, of which one CH₂group can be replaced by oxygen, S, NH, N—CH₃, N-benzyl orN-(p-chlorophenyl); or Z is an N-containing heterocycle having 1, 2, 3,4, 5, 6, 7, 8 or 9 carbon atoms, where the N-containing heterocycle islinked via N or C and is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, Br, CF₃,methyl, methoxy and NR(21)R(22); but where, in the case where R(4) is analkoxy radical, at least one of the substituents R(2), R(3), R(5), R(6),R(7) and R(8) is not hydrogen; or pharmaceutically tolerable saltthereof; ba) a substituted 2-naphthoylguanidine of the formula

in which: at least one of the substituents R1, R3, R4, R5, R6, R7 and R8is XY_(a)WZ or X′Y_(a)WZ′; X is O, S, NR(10) or CR(11)R(12); R(10),R(11) and R(12) independently of one another are H, alkyl having 1, 2,3, 4, 5 or 6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbonatoms or cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; Y is alkylenehaving 1, 2, 3, 4, 5, 6, 7 or 8 CH₂ groups, where one of these CH₂groups can be replaced by O, S, NR(13) or o-, p- or m-phenylene; R(13)is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3, 4, 5 or 6carbon atoms; a is zero or 1; W is CH₂, SO₂, S(═O)(═NH) or, if W doesnot immediately follow a heteroatom of the group Xy_(a), alternatively Oor NR(14); R(14) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5 or 6 carbon atoms; Z is C(═O)R(15), SO₂R(15) or, if W is not O orNR(14), alternatively NR(16)R(17); R(15) is N═C(NH₂)₂, NR(18)R(19),N(CH₂)_(b)NR(18)R(19) or OR(20); b is 2 or 3; R(18) and R(19)independently of one another are H, alkyl having 1, 2, 3, 4, 5, 6, 7 or8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; orR(18) and R(19) together are 4 or 5 methylene groups, of which one CH₂group can be replaced by oxygen, S, NH, N—CH₃, N-benzyl orN-(p-chlorophenyl); R(20) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbonatoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkylhaving 3, 4, 5, 6 or 7 carbon atoms; R(16) and R(17) independently ofone another are H, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms orperfluoroalkyl having 1, 2, 3 or 4 carbon atoms; or, R(16) and R(17)together are 4 or 5 methylene groups,  of which one CH₂ group can bereplaced by oxygen, S, NH, N—CH₃, N-benzyl or N-(p-chlorophenyl); X′ isC═O, C(═O)NR(30), C(═O)O, SO, SO₂, SO₂NR(30), OC═O, NR(30)C═O orNR(30)SO₂, where the linkage with the naphthalene ring in each casetakes place via the left atom; R(30) is H, alkyl having 1, 2, 3, 4, 5 or6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms orcycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; Z is C(═O)R(15),SO₂R(15), an N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or 9carbon atoms, where the N-containing heterocycle is linked via N or Cand is not substituted or is substituted by 1-3 substituents selectedfrom the group consisting of F, Cl, Br, CF₃, methyl, methoxy andNR(21)R(22); R(21) and R(22) independently of one another are H, alkylhaving 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4carbon atoms; R(15) is N═C(NH₂)₂, NR(18)R(19), N(CH₂)_(b)NR(18)R(19) orOR(20); R(18) and R(19)  independently of one another are H, alkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or perfluoroalkyl having 1,2, 3 or 4 carbon atoms; or R(18) and R(19)  together are 4 or 5methylene groups,  of which one CH₂ group can be replaced by oxygen, S,NH, N—CH₃, N-benzyl or N-(p-chlorophenyl); b is 2 or 3; R(20) is H,alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkyl having 1,2, 3 or 4 carbon atoms or cycloalkyl having 3, 4, 5, 6 or 7 carbonatoms; or Z′ if W is not O or NR(14), is NR(16)R(17); R(16) and R(17)independently of one another are H, alkyl having 1, 2, 3, 4, 5, 6, 7 or8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; orR(16) and R(17) together are 4 or 5 methylene groups,  of which one CH₂group can be replaced by oxygen, S, NH, N—CH₃, N-benzyl orN-(p-chlorophenyl); and the other substituents R1, R3, R4, R5, R6, R7and R8 in each case, which are still not allocated by the definitionsgiven above, independently of one another are H, F, Cl, Br, I, CN, NO₂,CF₃, C₂F₅ or V_(p)Q_(q)U; V is O, S, SO, SO₂, NR(60), OC═O, C═O,C(═O)NR(60), C(═O)O or CR(66)R(67); R(60), R(66) and R(67) independentlyof one another are H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms,perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3,4, 5, 6 or 7 carbon atoms; p is zero or 1; Q is alkylene having 1, 2, 3,4, 5, 6, 7 or 8 CH₂ groups, where one of these CH₂ groups can bereplaced by O, S, NR(68) or o-, p- or m-phenylene; R(68) is H, alkylhaving 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkyl having 1, 2, 3 or4 carbon atoms or cycloalkyl having 3, 4, 5 or 6 carbon atoms; q is zeroor 1; U is H, alkyl having 1, 2, 3, 4, 5, 6 or 7 carbon atoms,cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms, C(═O)R(65), SO₂R(65),NR(61)R(62) or phenyl, which is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, Br, CF₃,methyl, methoxy and NR(63)R(64); R(63) and R(64) independently of oneanother are H, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms; R(65) is N═C(NH₂)₂, NR(61)R(62) orOR(60); R(61) and R(62) independently of one another are H, alkyl having1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3or 4 carbon atoms; or R(61) and R(62) together are 4 or 5 methylenegroups,  of which one CH₂ group can be replaced by oxygen, S, NH, N—CH₃,N-benzyl or N-(p-chlorophenyl); or U is an N-containing heterocyclehaving 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, where the N-containingheterocycle is linked via N or C and is not substituted or issubstituted by 1-3 substituents selected from the group consisting of F,Cl, Br, CF₃, methyl, methoxy and NR(63)R(64); but where at least one ofthe substituents R5, R6, R7 and R8 is not hydrogen; or pharmaceuticallytolerable salt thereof; bb) an ortho-substituted benzoylguanidine of theformula

in which: R(1) is H, F, Cl, Br, I, CN, NO₂, alkyl having 1, 2, 3, 4, 5,6, 7 or 8 carbon atoms, alkoxy having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkoxyhaving 3, 4, 5, 6, 7 or 8 carbon atoms or X_(a)—(CH₂)_(b)—(CF₂)_(c)—CF₃;X is oxygen, sulfur or NR(9); a is zero or 1; b is zero, 1 or 2; c iszero, 1, 2 or 3; R(9) is H, alkyl having 1, 2, 3 or 4 carbon atoms or—C_(d)H_(2d)R(6); d is zero, 1, 2, 3 or 4; R(6) is cycloalkyl having 3,4, 5, 6, 7 or 8 carbon atoms, phenyl, biphenylyl or naphthyl,  where thearomatics phenyl, biphenylyl or naphthyl are not substituted or aresubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(7)R(8);  R(7) and R(8) are independently, H or alkyl having 1, 2, 3 or 4 carbon atoms; or R(1) is—SR(10), —OR(10) or —CR(10)R(11)R(12); R(10) is —C_(f)H_(2f)-cycloalkylhaving 3, 4, 5, 6, 7 or 8 carbon atoms in the cycloalkyl ring,heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms or phenyl,where heteroaryl and phenyl are unsubstituted or are substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethylamino; f is zero, 1 or2; R(11) and (R12), independently of each other, are defined as R(10) orare hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; or R(1) isphenyl, naphthyl, biphenylyl or heteroaryl having 1, 2, 3, 4, 5, 6, 7,8, or 9 carbon atoms, the latter linked via a carbon or nitrogen atom ofthe ring, each of which is unsubstituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, CH₃,methoxy, hydroxyl, amino, methylamino and dimethyl-amino, or R(1) is—SR(13), —OR(13), —NHR(13), —NR(13)R(14), —CHR(13)R(15),—C[R(15)R(16)OH], —C≡CR(18), —C[R(19)]═CHR(18) or—C[R(20)R(21)]_(k)—(CO)—[CR(22)R(23)]_(l)—R(24), k is zero, 1, 2, 3 or4; l is zero, 1, 2, 3 or 4; R(13) and R(14), identically or differently,are —(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(kk)—R(17) or—(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(24); R(17) is hydrogen or methyl, g, h andi,  identically or differently, are zero, 1, 2, 3 or 4; kk is 1, 2, 3 or4; R(15) and R(16), identically or differently, are hydrogen, alkylhaving 1, 2, 3, 4, 5 or 6 carbon atoms, or, together with the carbonatom carrying them, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms;R(18) is phenyl, which is unsubstituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy and NR(25)R(26); R(25) and R(26) are  H or alkyl having 1, 2, 3or 4 carbon atoms; or R(18) is heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8or 9 carbon atoms, which is unsubstituted or is substituted as phenyl;or R(18) is alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, which isunsubstituted or is substituted by 1-3 OH; or R(18) is cycloalkyl having3, 4, 5, 6, 7 or 8 carbon atoms; R(19), R(20), R(21), R(22) and R(23),identically or differently, are hydrogen or methyl; R(24) is H, alkylhaving 1, 2, 3, 4, 5 or 6 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7or 8 carbon atorms or —C_(m)H_(2m)—R(18); m is 1, 2, 3 or 4; one of thetwo substituents R(2) and R(3) is —O—CO—R(27); R(27) is alkyl having 1,2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms, phenyl, biphenylyl, naphthyl, pyridyl or quinolinyl, wherephenyl, biphenylyl, naphthyl, pyridyl or quinolyl are unsubstituted orsubstituted by 1-3 substituents selected from the group consisting of F,Cl, CF₃, methyl, methoxy and NR(7)R(8); R(7) and R(8) independently ofone another are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms;where one of the substituents R(2) and R(3) is always defined as R(1);R(4) and R(5) independently of one another are hydrogen, alkyl having 1,2, 3 or 4 carbon atoms, alkoxy having 1, 2, 3 or 4 carbon atoms, F, Cl,Br, I, CN or —(CH₂)_(n)—(CF₂)_(o)—CF₃, n is zero or 1, o is zero or 1,or pharmaceutically tolerable salt thereof; bc) a benzoylguanidine ofthe formula

in which: R(1) is R(13)—SO_(m) or R(14)R(15)N—SO₂—; m is 1 or 2; R(13)is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, perfluoroalkylhaving 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, alkenyl having 3, 4, 5, 6,7 or 8 carbon atoms or —C_(n)H_(2n)—R(16), n is zero, 1, 2, 3 or 4;R(16) is cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, phenyl,biphenylyl or naphthyl, where phenyl, biphenylyl and naphthyl are notsubstituted or are substituted by 1-3 substituents selected from thegroup consisting of F, Cl, CF₃, methyl, methoxy and NR(25)R(26); R(25)and R(26) are,  independently of each other, hydrogen, alkyl having 1,2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbonatoms; R(14) is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbonatoms, perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms,alkenyl having 3, 4, 5, 6, 7 or 8 carbon atoms or —C_(n)H_(2n)—R(27), nis zero, 1, 2, 3 or 4; R(27) is cycloalkyl having 3, 4, 5, 6, 7 or 8carbon atoms, phenyl, biphenylyl or naphthyl, where phenyl, biphenylyland naphthyl are not substituted or are substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(28)R(29); R(28) and R(29) are,  independently of each other,hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkylhaving 1, 2, 3 or 4 carbon atoms; R(15) is hydrogen, alkyl having 1, 2,3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms;or R(14) and R(15) are, together, 4 or 5 methylene groups of which oneCH₂ group can be replaced by oxygen, S, NH, N—CH₃ or N-benzyl; one ofthe substituents R(2) and R(3) is hydrogen; and the other of thesubstituents R(2) and R(3) in each case is —CHR(30)R(31); R(30) is—(CH₂)_(g)—(CHOH)_(h)—(CH₂)_(i)—(CHOH)_(k)—R(32) or—(CH₂)_(g)—O—(CH₂—CH₂O)_(h)—R(24); R(24) and R(32) are, independently ofeach other, hydrogen or methyl; g, h and i are, identically ordifferently, zero, 1, 2, 3 or 4; k is 1, 2, 3 or 4; or the other of thesubstituents R(2) and R(3) in each case is —C(OH)R(33)R(34); R(31),R(33) and R(34) are, identically or differently, hydrogen or alkylhaving 1, 2, 3 or 4 carbon atoms, or R(33) and R(34) are, together,cycloalkyl having 3, 4, 5 or 6 carbon atoms; or R(33) is —CH₂OH; R(4) isalkyl having 1, 2, 3 or 4 carbon atoms, alkoxy having 1, 2, 3 or 4carbon atoms, F, Cl, Br, I, CN or —(CH₂)_(n)—(CF₂)_(o)—CF₃; n is zero or1; o is zero, 1 or 2; or pharmaceutically tolerable salt thereof; bd) anindanylidineacetylguanidine of the formula

in which: R1, R2, R3, R4, R5 and R6 independently of one another are H,C₁-C₁₀-alkyl; haloalkyl having 1-6 carbon atoms, O—C₁-C₁₀-alkyl,haloalkoxy having 1-6 carbon atoms, F, Cl, Br, I, aryl, substitutedaryl, heteroaryl, substituted heteroaryl, OH, O-lower alkyl, O-aryl,O-lower alkylaryl, O-substituted aryl, O-lower alkyl-substituted aryl,O—C(═O)—C₁-C₄-alkylaryl, O—C(═O)—NH—C₁-C₄-alkyl,O—C(═O)—N(C₁-C₄-alkyl)₂, NO₂, CN, CF₃, NH₂, NH—C(═O)—C₁-C₄-alkyl,NH—C(═O)—NH₂, COOH, C(═O)—O—C₁-C₄-alkyl, C(═O)—NH₂,C(═O)—NH—C₁-C₄-alkyl, C(═O)—N(C₁-C₄-alkyl)₂, C₁-C₄—COOH,C₁-C₄-alkyl-C(═O)—O—C₁-C₄-alkyl, SO₃H, SO₂-alkyl; SO₂-alkylaryl,SO₂—N-(alkyl)₂, SO₂—N(alkyl)(alkylaryl), C(═O)—R11,C₁-C₁₀-alkyl-C(═O)—R11, C₂-C₁₀-alkenyl-C(═O)—R11,C₂-C₁₀-alkynyl-C(═O)—R11, NH—C(═O)—C₁-C₁₀-alkyl-C(═O)—R11 orO—C₁-C₁₁-alkyl-C(═O)—R11; R11 is C₁-C₄-alkyl, C₁-C₄-alkynyl, aryl,substituted aryl, NH₂, NH—C₁-C₄-alkyl, N-(C₁-C₄-alkyl)₂, SO₃H,SO₂-alkyl, SO₂-alkylaryl, SO₂—N-(alkyl)₂ or SO₂—N(alkyl)(alkylaryl); Xis O, S or NH; R7, R8, R9 and R10 independently of one another are H,alkyl, cycloalkyl, aryl, alkylaryl, or R8 and R9 together are part of a5-, 6- or 7-membered heterocyclic ring; or pharmaceutically acceptablesalt thereof; be) a phenyl-substituted alkenylcarboxylic acid guanidideof the formula

in which: T is

R(A) is hydrogen, F, Cl, Br, I, CN, OH, OR(6), (C₁-C₄)-alkyl,O_(r)(CH₂)_(a)C_(b)F_(2b+1), (C₃-C₈)-cycloalkyl or NR(7)R(8) r is zeroor 1; a is zero, 1, 2, 3 or 4; b is 1, 2, 3 or 4; R(6) is (C₁-C₄)-alkyl,(C₁-C₄)-perfluoroalkyl, (C₃-C₆)-alkenyl, (C₃-C₈)-cycloalkyl, phenyl orbenzyl, the phenyl nucleus not being substituted or being substituted by1-3 substituents selected from the group consisting of F, Cl, CF₃,methyl, methoxy and NR(9)R(10); R(9) and R(10)  are H, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoro-alkyl; R(7) and R(8)  independently of one another aredefined as R(6); or R(7) and R(8)  together are 4 or 5 methylene groups,of which one CH₂ group can be replaced by oxygen, sulfur, NH, N—CH₃ orN-benzyl; R(B), R(C) and R(D) independently are defined as R(A); x iszero, 1 or 2; y is zero, 1 or 2; R(F) is hydrogen, F, Cl, Br, I, CN,OR(12), (C₁-C₈)-alkyl, O_(p)(CH₂)_(f)C_(g)F_(2g+1), (C₃-C₈)-cycloalkylor (C₁-C₉)-heteroaryl; p is zero or 1; f is zero, 1, 2, 3 or 4; g is 1,2, 3, 4, 5, 6, 7 or 8; R(12) is (C₁-C₈)-alkyl, (C₁-C₄)-perfluoroalkyl,(C₃-C₈)-alkenyl, (C₃-C₈)-cycloalkyl, phenyl or benzyl, the phenylnucleus not being substituted or being substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl, methoxy andNR(13)R(14); R(13) and R(14)  are H, (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; R(E) is defined independently as R(F); R(1) isdefined independently as T; or R(1) is hydrogen, —O_(k)C_(m)H_(2m+1),—O_(n)(CH₂)_(p)C_(q)F_(2q+1), F, Cl, Br, I, CN, —(C═O)—N═C(NH₂)₂,—So_(r)R(17), —So_(r2)NR(31)R(32), —O_(u)(CH₂)_(v)C₆H₅,—O_(u2)—(C₁-C₉)-heteroaryl or —S_(u2)—(C₁-C₉)-heteroaryl; k is zero or1; m is zero, 1, 2, 3, 4, 5, 6, 7 or 8; n is zero or 1; p is zero, 1, 2,3 or 4; q is 1, 2, 3, 4, 5, 6, 7 or 8; r is zero, 1 or 2; r2 is zero, 1or 2; R(31) and R(32) independently of one another are hydrogen,(C₁-C₈)-alkyl or (C₁-C₈)-pernluoroalkyl; or R(31) and R(32) are,together, 4 or 5 methylene groups of which one CH₂ group can be replacedby oxygen, S, NH, N—CH₃ or N-benzyl; R(17) is (C₁-C₈)-alkyl; u is zeroor 1; u2 is zero or 1; v is zero, 1, 2, 3 or 4; where the phenyl nucleusis not substituted or is substituted by 1-3 substituents selected fromthe group consisting of F, Cl, CF₃, methyl, methoxy, —(CH₂),NR(21)R(22),NR(18)R(19) and (C₁-C₉)-heteroaryl; R(18), R(19), R(21) and R(22)independently of one another are (C₁-C₄)-alkyl or(C₁-C₄)-perfluoroalkyl; w is 1, 2, 3 or 4; where the heterocycle of the(C₁-C₉)-heteroaryl is unsubstituted or substituted by 1-3 substituentsselected from the group consisting of F, Cl, CF₃, methyl and methoxy;R(2), R(3), R(4) and R(5) independently of one another are defined asR(1), or R(1) and R(2) or R(2) and R(3) in each case together are—CH—CH═CH—CH—, which is not substituted or is substituted by 1-3substituents selected from the group consisting of F, Cl, CF₃, methyl,methoxy, —(CH₂)_(w2)NR(24)R(25) and NR(26)R(27); R(24), R(25), R(26) andR(27) are H, (C₁-C₄)-alkyl or (C₁-C₄)-perfluoroalkyl; w2 is 1, 2, 3 or4; the radical T being present in the molecule at least twice, but onlythree times at most; or pharmaceutically tolerable salt thereof; or bf)a benzoylguanidine of the formula

in which: R(1) is CF₃; one of the substituents R(2) and R(3) ishydrogen; and the other substituent R(2) or R(3) in each case is—C(OH)(CH₃)—CH₂OH, —CH(CH₃)—CH₂OH or —C(OH)(CH₃)₂; R(4) is methyl,methoxy, Cl or CF₃; or pharmaceutically tolerable salt thereof.
 3. Amethod as claimed in claim 1, wherein the inhibitor of the Na⁺/H⁺exchanger is: A. a compound of the formula

in which: W, Y and Z are a nitrogen atom or a carbon atom substituted byR(2) or R(3) or R(4); R(1) is hydrogen, A, Hal, —CF₃, —CH₂F, —CHF₂,—CH₂CF₃, —C₂F₅, —CN, —NO₂, -ethynyl, or an X—R′; A is alkyl having 1 to6 carbon atoms; Hal is F, Cl, Br or I; X is oxygen, S or NR″; R″ ishydrogen, A or a cyclic methylene chain having 3 to 7 carbon atoms; R′is H, A, HO—A—, HOOC—A—, (C₃-C₇)-cycloalkyl, (C₆-C₈)-cycloalkylalkyl,CF₃, CH₂F, CHF₂, CH₂—CF₃, Ph, —CH₂—Ph or Het; Ph is phenyl, naphthyl orbiphenylyl which is unsubstituted or mono-, di- or trisubstituted by A,OA, NR′R″, Hal or CF₃; Het is a mono- or binuclear saturated,unsaturated or aromatic heterocycle having 1 to 4 nitrogen, oxygen orsulfur atoms, which is unsubstituted or mono-, di- or trisubstituted byHal, CF₃, A, OH, OA, —X—R′, —CN, —NO₂, or carbonyl oxygen, where Het isbonded via N or an alkylene chain C_(m)H_(2m) where m=zero to 6; or R′and R″ together are alkylene having 4-5 carbon atoms, in which one CH₂group can also be replaced by oxygen, S, NH, N—A, N—Ph and N—CH₂—Ph;R(2) and R(3) independently of one another are hydrogen, Hal, A, HO—A—,X—R′, —C(═N—OH)—A, A—O—CO—(C₁-C₄)-alkyl-, CN, NO₂, COOH, CF₃, CH₂F,CHF₂, C₂F₅, CH₂CF₃, or S(O)_(n)R′″; R′″ is A, Ph or —Het; n is zero, 1or 2; or R(2) and R(3) independently of one another are SO₂NR′R″, Ph or—O—Ph, —O—CH₂—Ph, —CO—A, —CHO, —COOA, —CSNR′R″, CONR′R″, —CH═CH—COOH,—CH═CH—COOA, indenyl, indanyl, decahydronaphthyl, cyclopentenyl,dihydrothienyl, dihydrofuryl, heterobicyclyl, alkylthienyl, halothienyl,haloalkylthienyl, acylthienyl, halofuryl, haloalkylfuryl or pyrrolyl; orR(2) and R(3) independently of one another are R(5)—O—; R(5) ishydrogen, A, (C₁-C₆)-alkenyl or (C₃-C₇)-cycloalkyl; R(4) is Ph, Het,—O-Het; CF₃, S(O)_(r)R′″, —SO₂NR′R″, alk;

 or  two of the substituents R(1) to R(4) together are a group—O—CR(6)R(7)—CO—NR(8)—,

where R(2) has the meaning indicated; R(6), R(7), R(8) and R(9)independently of one another are H or A; or R(8) is (C₅-C₇)-cycloalkyl;or R(9) is cyano; alk is straight-chain or branched (C₁-C₈)-alkyl or(C₃-C₈)-cycloalkyl, which is unsubstituted or mono-, di- ortrisubstituted by A; or alk is an ethenyl or ethynyl radical which issubstituted by H, A, Ph or Het; B. a compound of the formula

in which: X is H, Hal, (Hal)₃C—, (C₁-C₆)-alkyl, (C₃-C₆)-cycloalkyl,substituted phenyl, (C₁-C₅)-alkyl-S— or (C₁-C₅)-alkyl-SO₂—; Y is NH₂ orsubstituted amino; or X and Z together are a —(CH₂)₄— or a1,3-butadienylene chain; or Z is H, Hal, OH, HS, (C₁-C₅)-alkyl,(C₃-C₆)-cycloalkyl or substituted phenyl; or Z is an amino group—NR(1)R(2); R(1) is H, straight- and branched-chain, optionallysubstituted (C₁-C₈)-alkyl, which can be interrupted by oxygen; or R(1)is (C₃-C₈)-alkenyl, (C₃-C₈)-alkynyl, (C₃-C₇)-cycloalkyl orOH-substituted phenyl or OH-substituted phenyl-(C₁-C₄)-alkyl orOH-substituted (C₃-C₇)-cycloalkyl; R(2) is 1-morpholino, hydrogen or astraight or branched (C₁-C₈)-alkyl chain, which can be interrupted byoxygen or an amino group, which straight or branched (C₁-C₈)-alkyl chainis unsubstituted or substituted by a substituted or unsubstituted mono-or polynuclear heterocycle which contains a nitrogen, oxygen or sulfuratom; or which alkyl chain is substituted by phenyl, optionally mono- orpolysubstituted by (C₁-C₄) alkoxy, optionally substituted by OH,alkylamino, alkyl or phenyl; or by an aminocarbonyl group or by hydroxylor (C₁-C₄)-alkoxy group, or R(2) is phenyl, unsubstituted or substitutedby alkyl, alkoxy or an amino group, which as substituents carries: H, amono- or polynuclear heterocycle which contains a nitrogen, oxygen orsulfur atom,  which is unsubstituted or substituted by H, Hal or(C₁-C₄)-alkyl; or a phenyl radical,  unsubstituted or substituted by asubstituent selected from the group consisting of (C₁-C₄)-alkyl,(C₁-C₄)-alkoxy, Hal and OH; or R(2) is 1-piperidino, unsubstituted orsubstituted in the 4-position by an acyl radical of an aliphatic,alicyclic, aromatic or heteroaromatic carboxylic acid, (C₁-C₈) alkyl,which for its part can be substituted by OH or (C₁-C₄)-alkoxy or a(C₁-C₄)-alkoxy-substituted phenyl radical; or R(2) is amidino, which isunsubstituted or substituted by phenyl, which is unsubstituted orsubstituted by Hal or alkyl; or R(2) is an acyl radical of an aliphatic,alicyclic, aromatic or heteroaromatic carboxylic acid, or R(2) is a(C₁-C₈) alkyl chain, which can be substituted by a phenyl radicalcarrying an OH, alkoxy or alkyl radical; or R(1) and R(2) together withthe nitrogen atom to which they are bonded, are a piperazine ring, whichis unsubstituted or, via a (C₁-C₆)-methylene chain, carries a mono- orpolynuclear heterocycle,  which contains nitrogen, oxygen or sulfur Halis F, Cl, Br or I; C. an indoloylguanidine derivative of the formula

in which R(2) is hydrogen, unsubstituted or substituted (C₁-C₈)-alkyl,(C₃-C₇)-cycloalkyl, OH, (C₁-C₆)-alkyl-O—, an aromatic radical or a group—CH₂—R(20); R(20) is (C₂-C₆)-alkenyl or (C₂-C₆)-alkynyl; R(1) is 1 to 5identical or different substituents, which are: hydrogen, unsubstitutedor substituted (C₁-C₈)-alkyl, (C₂-C₆)-alkenyl, (C₂-C₆)-alkynyl,(C₃-C₇)-cycloalkyl, halogen, —NO₂, (C₂-C₈)-alkanoyl, arylalkanoyl havingup to 10 carbon atoms, aroyl having up to 11 carbon atoms, —COOH,(C₂-C₆)-alkoxycarbonyl, an aromatic group or one of the followingmentioned groups: —OR(3), —NR(6)R(7) or —S(O)_(n)R(40); R(3) ishydrogen, (C₁-C₈)-alkyl, substituted (C₁-C₈)-alkyl, (C₃-C₇)-cycloalkyl,an aromatic radical or a group —CH₂—R(30); R(30) is alkenyl or alkynyl;R(6) and R(7) independently of one another are hydrogen, unsubstitutedor substituted (C₁-C₈)-alkyl, (C₃-C₇)-cycloalkyl, (C₂-C₈)-alkanoyl, anarylalkanoyl group having up to 10 carbon atoms, an aroyl group havingup to 11 carbon atoms, an aromatic group or —CH₂—R(60); R(60) is(C₂-C₆)-alkenyl or (C₂-C₆)-alkynyl; or R(6) and R(7) together with thenitrogen atom are a 5-7-membered cyclic amine, which can additionallycontain further heteroatoms in the ring; n is zero, 1 or 2; R(40) isunsubstituted or substituted (C₁-C₈)-alkyl, or an aromatic group, or agroup

A is oxygen, —S(O)_(n)— or —NR(50)—; R(50) is hydrogen or (C₁-C₈)-alkyl;R′ is hydrogen, unsubstituted or substituted (C₁-C₈)-alkyl, in which thering represents a saturated 3-8-membered heterocycle having a nitrogenatom, said substituted alkyl carries one or more groups selected fromthe group consisting of halogen, —OH, (C₁-C₆)-alkoxy, —CN, —COOH,(C₂-C₆)-alkoxycarbonyl, (C₂-C₈)-alkanoyl, arylalkanoyl having up to 10carbon atoms, aroyl having up to 11 carbon atoms, an aromatic group and—CONR(4)R(5), R(4) and R(5) identically or differently are hydrogen or(C₁-C₈)-alkyl; or R(4) and R(5) are connected to one another andtogether form a 5-7-membered cyclic amine which can additionally containfurther heteroatoms in the ring, or said substituted alkyl carries agroup

 in which: E is a nitrogen atom or a CH group; R″ is hydrogen,(C₁-C₈)-alkyl which is unsubstituted or substituted by OH or substituted(C₁-C₈)-alkyl, (C₁-C₆)-alkoxy, —CN, —COOH, (C₂-C₆)-alkoxycarbonyl,(C₂-C₈)-alkanoyl, aralkanoyl having up to 10 carbon atoms, aroyl havingup to 11 carbon atoms, an aromatic group, —NR(6)R(7) or —CONR(4)R(5);R(4) and R(5)  independently of one another are hydrogen or(C₁-C₈)-alkyl; where the cyclic system of the formula

is a 3-8-membered saturated aliphatic or heterocyclic ring system havinga nitrogen atom, and where the aromatic groups mentioned are an arylradical having up to 10 carbon atoms, a 5- or 6-membered heteroarylradical having 1-4 nitrogen atoms, a 5- or 6-membered heteroaryl groupcontaining 1 or 2 nitrogen atoms and a heteroatom which is oxygen orsulfur, or furyl, and where the aryl radicals mentioned can beunsubstituted or substituted by unsubstituted (C₁-C₈)-alkyl orsubstituted (C₁-C₈)-alkyl, halogen, —NO₂, (C₂-C₆)-alkoxycarbonyl, COOH,—OR(3), NR(6)R(7), —CONR(4)R(5), —SO₂NR(6)R(7) or S(O)_(n)R(40), whereR(1) and the guanidinocarbonyl radical can be in any desired position ofthe 5- or 6-membered ring of the indole system, or pharmaceuticallytolerable salt thereof; D. a heterocyclic guanidine derivative of theformula

in which: X is —O—, —S—, —NH—, —N[(C₁-C₄)-alkyl]- or —N(phenyl)-; R(1),R(2) and R(3) are hydrogen, halogen, (C₁-C₄)-alkyl, (C₁-C₄)-alkyl-O—,phenyl or benzyl; or two of the substituents R(1), R(2) and R(3)together with one side of the benzo system are a 4-6-memberedcarbocyclic ring; R(4) and R(5) independently of one another arehydrogen, (C₁-C₁₂)-alkyl, benzhydryl, aralkyl, which is unsubstituted orsubstituted by one or more substituents from the groups halogen,(C₁-C₄)-alkyl, (C₁-C₄)-alkyl-O—, —CF₃ and —(CH₂)_(m)—CH₂—T, m is zero to3; T is —CO—O—T(1); T(1) is hydrogen or (C₁-C₄)-alkyl; Cy is abenzo-fused unsaturated or dihydro-5-membered ring heterocycle

 a pyrazole or imidazole ring of the formula

 a naphthyl radical or a dihydro- or tetrahydronaphthyl radical

 a 2-, 3- or 4-pyridyl radical

Z is N— or CH; a thienyl radical

R(6) is hydrogen, halogen, hydroxyl, (C₁-C₁₀)-alkyl, (C₁-C₁₀)-alkyl-O—,phenoxy, (C₁-C₁₀)-alkyloxymethyloxy- or —(O)_(n)S—R(9); n is zero, 1 or2; R(9) is (C₁-C₁₀)-alkyl, thienyl, pyridyl, thiazolyl, thiadiazolyl,imidazolyl, pyrazolyl or phenyl, each of which is unsubstituted or mono-or disubstituted by halogen, (C₁-C₄)-alkyl or (C₁-C₄)-alkyl-O—; R(7) andR(8) are hydrogen, halogen, hydroxyl, (C₁-C₁₀)-alkyl, (C₁-C₁₀)-alkyl-O—,phenyl, phenoxy or (C₁-C₁₀)-alkoxymethyloxy; or Cy is phenyl, which isunsubstituted or is mono- or disubstituted by halogen, (C₁-C₄)-alkyl or(C₁-C₄)-alkyl-O—; or Cy is —Gr—Am; Gr is—R(13)—R(12)—(CH₂)_(q)—C[W][W(1)]—(CH₂)_(q′)—; R(13)R(14)— or —R(15)—;R(12) is a single bond, —O—, —(O)_(n)S—, —CO— or —CONH—; n is zero, 1 or2; R(13) is a single bond, phenyl, thienyl, pyridyl, thiazolyl,thiadiazolyl, imidazolyl or pyrazolyl; R(14) is a single bond or SO₂—;R(15) is (C₂-C₁₀)-alkenyl or (C₂-C₁₀)-alkynyl; W and W(1) independentlyof one another are hydrogen, (C₁-C₄)-alkyl; or W and W(1) cyclicallyconnected to one another are a (C₃-C₈)-hydrocarbon ring; q and q′ arezero to 9; Am is —NR(10)R(11); R(10) is hydrogen, (C₁-C₄)-alkyl orbenzyl, R(11) is (C₁-C₄)-alkyl, phenyl or benzyl; or R(10) and R(11)together are a (C₃-C₁₀)-alkylene group,  which is unsubstituted orsubstituted by —COOH, (C₁-C₅)-alkoxycarbonyl, (C₂-C₄)-hydroxylalkyleneor benzyl; or Am is pyrrolyl, pyridyl, pyrazolyl, morpholinyl,dihydropyridyl, tetrahydropyridyl, quinuclidinyl, imidazolyl or3-azabicyclo[3.2.1 ]octyl, which is unsubstituted or substituted by(C₁-C₄)-alkyl, or Am is azabicyclo[3.2.2]nonyl; or Am is a piperazinegroup of the formula

R(16) is hydrogen, (C₁-C₄)-alkyl, (C₃-C₆)-cycloalkyl,phenyl, tolyl,methoxyphenyl, halophenyl, diphenylmethylene, benzyl or pyridyl; or Amis an azido group —(O)_(t)—(CH₂)_(q)—C[W][W(1)]—(CH₂)_(q)—N₃; t is zeroor 1; where W and W(1) have the previously indicated meaning; or anoptical enantiomer thereof, or pharmacologically tolerable salt thereof;or E. a guanidine compound of the formula

where R1=R2 is H, halo, alkyl, CN, NO₂, perfluoroalkyl, or SO_(n)CF₃; R3is CH═CH₂, CH₂—CH═CH₂, CH₂—CH₂—CH═CH₂, cycloalkenyl, orcycloalkenylalkyl; n is zero, 1 or 2; and R4 is alkyl, substitutedphenyl, or unsubstituted phenyl.
 4. A method as claimed in claim 1,wherein the inhibitor of the Na⁺/H⁺ exchanger is a guanidine compound.5. A method as claimed in claim 1, wherein the inhibitor of the Na⁺/H⁺exchanger is a cariporide.
 6. A method as claimed in claim 1, whereinthe disturbance of the central nervous system is hyperexcitability ofneurons occurring under a nonischemic condition.
 7. A method as claimedin claim 2, wherein the disturbance of the central nervous system ishyperexcitability of neurons occurring under a nbnischemic condition. 8.A method as claimed in claim 3, wherein the disturbance of the centralnervous system is hyperexcitability of neurons occurring under anonischemic condition.
 9. A method as claimed in claim 4, wherein thedisturbance of the central nervous system is hyperexcitability ofneurons occurring under a nonischemic condition.
 10. A method as claimedin claim 5, wherein the disturbance of the central nervous system ishyperexcitability of neurons occurring under a nonischemic condition.11. A method as claimed in claim 1, wherein the disturbance of thecentral nervous system is an epilepsy occurring under a nonischemiccondition.
 12. A method as claimed in claim 2, wherein the disturbanceof the central nervous system is an epilepsy occurring under anonischemic condition.
 13. A method as claimed in claim 3, wherein thedisturbance of the central nervous system is an epilepsy occurring undera nonischemic condition.
 14. A method as claimed in claim 4, wherein thedisturbance of the central nervous system is an epilepsy occurring undera nonischemic condition.
 15. A method as claimed in claim 5, wherein thedisturbance of the central nervous system is an epilepsy occurring undera nonischemic condition.
 16. A method as claimed in claim 1, wherein thedisburbance of the central nervous system is an affective psychosis oranxiety disorder occurring under a nonischemic condition.
 17. A methodas claimed in claim 2, wherein the disburbance of the central nervoussystem is an affective psychosis or anxiety disorder occurring under anonischemic condition.
 18. A method as claimed in claim 3, wherein thedisburbance of the central nervous system is an affective psychosis oranxiety disorder occurring under a nonischemic condition.
 19. A methodas claimed in claim 4, wherein the disburbance of the central nervoussystem is an affective psychosis or anxiety disorder occurring under anonischemic condition.
 20. A method as claimed in claim 5, wherein thedisburbance of the central nervous system is an affective psychosis oranxiety disorder occurring under a nonischemic condition.